Search Result
Results for "
high oral bioavailability
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-15043
-
|
Bradykinin Receptor
|
Inflammation/Immunology
Endocrinology
|
ELN-441958 is a potent, neutral, competitive and selective bradykinin B1 receptor antagonist with a Ki of 0.26 nM against native human bradykinin B1 receptor. ELN-441958 has high oral bioavailability, and has low CNS exposure in the mouse .
|
-
-
- HY-151360
-
|
Sodium Channel
|
Metabolic Disease
|
NHE3-IN-3 (Compound 1) is a Na +/H + exchanger isoform 3 (NHE3) inhibitor with pIC50 of 6.2 and 6.6 against human and rat NHE3, respectively. NHE3-IN-3 shows high (98%) oral bioavailability in Sprague–Dawley rats .
|
-
-
- HY-161061
-
|
Arginase
|
Cancer
|
Arginase inhibitor 7 (compound A17) is an arginase (ARG1) inhibitor, with an IC50 of 0.16 μM. Arginase inhibitor 7 has high oral bioavailability .
|
-
-
- HY-120634
-
|
HCV
|
Infection
|
BMS-929075 is a potent and orally active HCV NS5B replicase palm site allosteric inhibitor. BMS-929075 shows high oral bioavailability. BMS-929075 shows cytotoxicity .
|
-
-
- HY-101699A
-
|
MCHR1 (GPR24)
|
Metabolic Disease
|
AMG-076 is an orally bioavailable and selective MCHR1 antagonist. AMG-076 results in significant reduction in body weight gain in nonobese mice fed a high-fat diet and in high-fat diet-induced obese (DIO) mice .
|
-
-
- HY-146223
-
|
Ras
|
Cancer
|
AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability .
|
-
-
- HY-135230
-
FP3FBZ
|
Opioid Receptor
|
Neurological Disease
|
LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects .
|
-
-
- HY-149345
-
|
IRAK
|
Inflammation/Immunology
|
IRAK4-IN-24 (compound 16) is a potent IRAK4 inhibitor, with high clearance (Cl) and poor oral bioavailability. IRAK4-IN-24 can be used for research in inflammatory and autoimmune disorders.
|
-
-
- HY-15023
-
PF-3274167
|
Oxytocin Receptor
|
Endocrinology
|
Cligosiban (PF-3274167), a high oral bioavailability and good brain-penetrant non-peptide oxytocin receptor antagonist, shows a high-affinity (Ki=9.5 nM) and an excellent selectivity versus the vasopressin receptors with almost no affinity for the V1b and V1a subtypes. Cligosiban inhibits ejaculatory physiology in rodents .
|
-
-
- HY-144878
-
|
c-Myc
|
Cancer
|
VPC-70619 is a potent, orally active N-Myc inhibitor. VPC-70619 blocks the N-Myc-Max heterocomplex from binding to DNA E-boxes and demonstrated strong inhibition activity against N-Myc-dependent cell lines as well as high bioavailability in both oral and intraperitoneal administration .
|
-
-
- HY-127105A
-
LNP023 hydrochloride
|
Complement System
|
Metabolic Disease
Inflammation/Immunology
|
LNP023 hydrochloride is an orally bioavailable, highly potent and highly selective factor B inhibitor. LNP023 shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. LNP023 inhibits factor B with an IC50 value of 10 nM .
|
-
-
- HY-15419
-
|
5-HT Receptor
|
Neurological Disease
|
RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .
|
-
-
- HY-15419A
-
|
5-HT Receptor
|
Neurological Disease
|
RS-127445 is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .
|
-
-
- HY-156593
-
|
ROCK
|
Cancer
|
ROCK-IN-9 (Compound T345) is a ROCK inhibitor. ROCK-IN-9 shows cytotoxicity in HepG2 cell, with an IC50 of 40.8 μM. ROCK-IN-9 has good pharmacokinetic properties in mice, and shows high in vivo exposure and oral bioavailability at lower doses .
|
-
-
- HY-B0717
-
TPGS; D-α-Tocopherol polyethylene glycol 1000 succinate; Vitamin E-TPGS
|
Others
|
Neurological Disease
Metabolic Disease
|
Tocofersolan is synthetic polyethylene glycol derivative of α-tocopherol. Tocofersolan is an orally active and water-soluble analog of vitamin E. Tocofersolan can reduce neurobehavioral deficits in zebrafish embryos exposed to moderate and high concentrations of BaP during early development. Tocofersolan shows antioxidant activity. Tocofersolan can be used to provide an orally bioavailable source of vitamin E .
|
-
-
- HY-15010
-
|
Oxytocin Receptor
Vasopressin Receptor
|
Endocrinology
|
L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM) .
|
-
-
- HY-127105
-
LNP023
|
Complement System
|
Metabolic Disease
Inflammation/Immunology
|
Iptacopan (LNP023) is a first-in-class, orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 value of 10 nM. Iptacopan shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. Iptacopan targets the underlying cause of complement 3 glomerulopathy (C3G) .
|
-
-
- HY-153256
-
|
Prostaglandin Receptor
|
Metabolic Disease
|
EP3 antagonist 4 (Compound 28) is an EP3 antagonist, with a Ki value of 2 nM for hEP. EP3 antagonist 4 shows low in vivo clearance, high oral AUC, and good bioavailability in the rat full PK studies. EP3 antagonist 4 can be used for research of beta cell dysfunction in diabetes .
|
-
-
- HY-133747
-
|
JAK
|
Inflammation/Immunology
|
JAK3-IN-9 is an orally active JAK3 inhibitor with IC50 value of 1.7 nM. JAK3-IN-9 is highly selective to the JAK3 signal path. JAK3-IN-9 is lowly toxic with high oral bioavailability, shows good anti-arthritis activity. JAK3-IN-9 can be used in autoimmune disease research .
|
-
-
- HY-126321
-
|
ROR
|
Cancer
|
RORγt agonist 1 (compound 14) is a potent, orally bioavailable RORγt agonist with an EC50 of 20.8 nM. RORγt agonist 1 showes high metabolic stability, improved aqueous solubility and excellent mouse PK profile. RORγt agonist 1 is a potential candidate of RORγt agonist for cancer immunotherapy .
|
-
-
- HY-100555
-
|
HSP
|
Infection
Cancer
|
CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model .
|
-
-
- HY-111925
-
|
TRP Channel
|
Cardiovascular Disease
|
BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7 .
|
-
-
- HY-146223A
-
|
Others
|
Cancer
|
(3R,10R,14aS)-AZD4625 is the isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability .
|
-
-
- HY-124634
-
PZ-2891
1 Publications Verification
|
Others
|
Neurological Disease
|
PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively .
|
-
-
- HY-109118A
-
SUVN-502 mesylate
|
5-HT Receptor
|
Neurological Disease
|
Masupirdine mesylate (SUVN-502 mesylate) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine mesylate (SUVN-502 mesylate) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease .
|
-
-
- HY-109118
-
SUVN-502 free base
|
5-HT Receptor
|
Neurological Disease
|
Masupirdine free base (SUVN-502 free base) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine free base (SUVN-502 free base) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease .
|
-
-
- HY-123857
-
|
P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
JNJ-55308942 is a high-affinity, selective, brain-penetrant P2X7 functional antagonist (hP2X7: IC50=10 nM, Ki=7.1 nM; rP2X7: IC50=15 nM, Ki=2.9 nM). JNJ-55308942 is orally bioavailable, binds to brain P2X7 and blocks IL-1β release from adult rodent brain .
|
-
-
- HY-148825
-
-
-
- HY-111790
-
M3258
1 Publications Verification
|
Proteasome
Apoptosis
|
Cancer
|
M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells .
|
-
-
- HY-120184
-
AZ13713945
|
mAChR
|
Neurological Disease
|
VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity .
|
-
-
- HY-13238
-
Dolutegravir
Maximum Cited Publications
20 Publications Verification
S/GSK1349572
|
HIV Integrase
HIV
|
Infection
|
Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
|
-
-
- HY-153460
-
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
TLR7/8/9 antagonist 2 is an orally active TLR7/8/9 antagonist. TLR7/8/9 antagonist 2 has inhibitory activities for HEK/hTLR7, HEK/hTLR8 and HEK/hTLR9 with IC50 values of 0.011 μM, 0.029 μM and 0,052 μM, respectively.TLR7/8/9 antagonist 2 has high bioavailability in vivo.TLR7/8/9 antagonist 2 can be used for the research of auto-inflammatory diseases such as systemic lupus erythematosus or lupus nephritis .
|
-
-
- HY-13238A
-
S/GSK1349572 sodium
|
HIV Integrase
HIV
|
Infection
|
Dolutegravir sodium (S/GSK1349572 sodium) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium (S/GSK1349572 sodium) retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
|
-
-
- HY-13238S1
-
S/GSK1349572-d3
|
Isotope-Labeled Compounds
HIV Integrase
HIV
|
Infection
|
Dolutegravir-d3 is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
|
-
-
- HY-13238S2
-
S/GSK1349572-d5
|
Isotope-Labeled Compounds
HIV Integrase
HIV
|
Infection
|
Dolutegravir-d5 is deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
|
-
-
- HY-13238R
-
|
HIV Integrase
HIV
|
Infection
|
Dolutegravir (Standard) is the analytical standard of Dolutegravir. This product is intended for research and analytical applications. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
|
-
-
-
HY-L061
-
|
3,555 compounds
|
Most of the drugs that are available in the marketplace are administered via the oral route, which is a convenient and cost effective route of administration. Thus, oral bioavailability is one of the key considerations in drug design and development. A high oral bioavailability reduces the amount of an administered drug necessary to achieve a desired pharmacological effect and therefore could reduce the risk of side-effects and toxicity. A poor oral bioavailability can result in low efficacy and higher inter-individual variability and therefore can lead to unpredictable response to a drug. Low oral bioavailability in clinical trials is a major reason for drug candidates failing to reach the market.
MCE offers a unique collection of 3,555 compounds with confirmed high oral bioavailability. MCE Orally Active Compound Library is a useful tool for discovering new drugs with oral bioavailability.
|
-
-
HY-L0121V
-
|
10,000 compounds
|
Natural products are an attractive source with varied structures that exhibit potent biological activities, and desirable pharmacological profiles. The core scaffold of a natural product can also provide a biologically validated framework upon which to display diverse functional groups. Inspired by bioactive natural products, natural product-like compounds, occupying the same chemical space, are ideally suited to explore and to facilitate understanding of biological pathways.
MCE 10K Natural Product-like Compound Library consists of 10,000 natural product-like compounds. Each compound has scaffold of natural products or Tanimoto coefficient >0.6 with natural products. The natural-likeness scoring of these compounds is >-2. What’s more, compounds in the library are drug-like and readily available for re-supply, making it a powerful tool for new drug research and development. It can be widely applied in high-throughput screening (HTS) and high-content screening (HCS).
|
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-13238S1
-
|
Dolutegravir-d3 is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
|
-
-
- HY-13238S2
-
|
Dolutegravir-d5 is deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
|
-
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent: