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GS-6201

Catalog No. T15418 CAS 752222-83-6

Synonyms: CVT-6883

GS-6201 (CVT-6883) is a selective antagonist of adenosine A2B receptor. GS-6201 shows high affinity and selectivity for the human adenosine A2B receptors with a Ki of 22 nM.

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GS-6201, CAS 752222-83-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 37.00
5 mg	In stock	$ 96.00
10 mg	In stock	$ 155.00
25 mg	In stock	$ 328.00
50 mg	In stock	$ 522.00
100 mg	In stock	$ 759.00
1 mL * 10 mM (in DMSO)	In stock	$ 117.00

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Purity: 99.74%

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Description	GS-6201 (CVT-6883) is a selective antagonist of adenosine A2B receptor. GS-6201 shows high affinity and selectivity for the human adenosine A2B receptors with a Ki of 22 nM.
Targets&IC50	A2B:22 nM(Ki, human), A3:1070 nM(Ki, human), A1:1940 nM(Ki, human), A2A:3280 nM(Ki, human)
In vivo	GS-6201 (2 mg/kg; p.o.) treatment displays the Cmax, dAUC and t1/2 are 1110 ng/mL, 6500 ng h/mL, and 4.25 hours, respectively [1]. GS-6201 (4 mg/kg; i.p.; every 12 h for 14 days) obviously decreases IL-6, TNF-α, E-selectin, ICAM-1, and VCAM plasma levels. GS-6201 (4 mg/kg; i.p.; every 12 h for 14 days) causes an obvious attenuation of left and right ventricular enlargement and dysfunction at 7 days, which was maintained at 14 days and also at 28 days [2].

Synonyms	CVT-6883
Molecular Weight	446.43
Formula	C21H21F3N6O2
CAS No.	752222-83-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/ml (67.2 mM), Sonication and heating to 60℃ are recommended.

References and Literature

1. Toldo S, et al. GS-6201, a selective blocker of the A2B adenosine receptor, attenuates cardiac remodeling after acute myocardial infarction in the mouse. J Pharmacol Exp Ther. 2012 Dec;343(3):587-95. 2. Mustafa SJ, et al. Effect of a specific and selective A(2B) adenosine receptor antagonist on adenosine agonist AMP and allergen-induced airway responsiveness and cellular influx in a mouse model of asthma. J Pharmacol Exp Ther. 2007 Mar;320(3):1246-51. 3. Elzein E, et al. Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases. J Med Chem. 2008 Apr 10;51(7):2267-78.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Membrane Protein-targeted Compound Library GPCR Compound Library ReFRAME Related Library Neurotransmitter Receptor Compound Library Bioactive Compound Library Neuronal Signaling Compound Library Bioactive Compounds Library Max Pyroptosis Compound Library

Related Products

Related compounds with same targets

Norisoboldine MRS 1754 APNEA BAY-545 VUF 5574 Adenosine receptor antagonist 4 Amp579 TFA Adenosine antagonist-1

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Keywords

GS-6201 752222-83-6 GPCR/G Protein Neuroscience Adenosine Receptor GS 6201 GS6201 Inhibitor remodeling cardiac caspase-1 reactivity airway affinity infarction P1 receptor CVT-6883 inhibit CVT6883 acute CVT 6883 selectivity myocardial inhibitor

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