2. GPCR/G Protein
  3. Prostaglandin Receptor
  4. TG8-260

TG8-260 is a second-generation EP2 antagonist developed to alleviate the pathology of central nervous system and peripheral diseases driven by inflammation. TG8-260 can reduce neuroinflammation and gliosis in the hippocampus of rats after pilocarpine-induced persistent epileptic status. Pharmacokinetic data of TG8-260 showed that its plasma half-life was 2.14 hours and its oral bioavailability was 77.3%. TG8-260 is also a potent inhibitor of CYP450 and shows antagonistic activity in inhibiting EP2 receptor-mediated inflammatory gene expression in BV2-hEP2 microglia, which is suitable for studying anti-inflammatory pathways in animal models of peripheral inflammatory diseases.

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TG8-260 Chemical Structure

TG8-260 Chemical Structure

CAS No. : 2490544-50-6

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10 mg USD 128 In-stock
25 mg USD 250 In-stock
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Description

TG8-260 is a second-generation EP2 antagonist developed to alleviate the pathology of central nervous system and peripheral diseases driven by inflammation. TG8-260 can reduce neuroinflammation and gliosis in the hippocampus of rats after pilocarpine-induced persistent epileptic status. Pharmacokinetic data of TG8-260 showed that its plasma half-life was 2.14 hours and its oral bioavailability was 77.3%. TG8-260 is also a potent inhibitor of CYP450 and shows antagonistic activity in inhibiting EP2 receptor-mediated inflammatory gene expression in BV2-hEP2 microglia, which is suitable for studying anti-inflammatory pathways in animal models of peripheral inflammatory diseases[1].

IC50 & Target

EP2[1]
Molecular Weight

344.41

Formula

C21H20N4O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=CC=C(C2=CN=CN2)C=C1)NCCC3=C(C)NC4=C3C=CC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (362.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9035 mL 14.5176 mL 29.0352 mL
5 mM 0.5807 mL 2.9035 mL 5.8070 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9035 mL 14.5176 mL 29.0352 mL 72.5879 mL
5 mM 0.5807 mL 2.9035 mL 5.8070 mL 14.5176 mL
10 mM 0.2904 mL 1.4518 mL 2.9035 mL 7.2588 mL
15 mM 0.1936 mL 0.9678 mL 1.9357 mL 4.8392 mL
20 mM 0.1452 mL 0.7259 mL 1.4518 mL 3.6294 mL
25 mM 0.1161 mL 0.5807 mL 1.1614 mL 2.9035 mL
30 mM 0.0968 mL 0.4839 mL 0.9678 mL 2.4196 mL
40 mM 0.0726 mL 0.3629 mL 0.7259 mL 1.8147 mL
50 mM 0.0581 mL 0.2904 mL 0.5807 mL 1.4518 mL
60 mM 0.0484 mL 0.2420 mL 0.4839 mL 1.2098 mL
80 mM 0.0363 mL 0.1815 mL 0.3629 mL 0.9073 mL
100 mM 0.0290 mL 0.1452 mL 0.2904 mL 0.7259 mL
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TG8-260 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TG8-2602490544-50-6Prostaglandin ReceptorAnti-InflammatoryEP2CYP450BV2-hEP2 cellInhibitorinhibitorinhibit

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