1. GPCR/G Protein
  2. Adenosine Receptor
  3. GS-6201

GS-6201 (Synonyms: CVT-6883)

Cat. No.: HY-10081 Purity: >98.0%
Handling Instructions

GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM). GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse. GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice.

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GS-6201 Chemical Structure

GS-6201 Chemical Structure

CAS No. : 752222-83-6

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10 mM * 1 mL in DMSO USD 309 In-stock
Estimated Time of Arrival: December 31
5 mg USD 315 In-stock
Estimated Time of Arrival: December 31
10 mg USD 540 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM)[1]. GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse[2]. GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice[3].

IC50 & Target

Ki: 22 nM (human A2B receptors), 1070 nM (human A3 receptors), 1940 nM (human A1 receptors), 3280 nM (human A2A receptors)[1]

In Vivo

GS-6201 (CVT-6883) (4 mg/kg; i.p.; every 12 h for 14 days) significantly reduces IL-6, TNF-α, E-selectin, ICAM-1, and VCAM plasma levels[2].
GS-6201 (4 mg/kg; i.p.; every 12 h for 14 days) leads to a significant attenuation of left and right ventricular enlargement and dysfunction at 7 days, which was maintained at 14 days and also at 28 days[2].
GS-6201 (2 mg/kg; p.o.) treatment shows the Cmax, dAUC and t1/2 are 1110 ng/mL, 6500 ng h/mL, and 4.25 hours, respectively[1].

Animal Model: Adult out-bred male CD1 mice (8-12 weeks of age, AMI model)[2]
Dosage: 4 mg/kg
Administration: i.p.; every 12 h for 14 days
Result: Significantly reduced IL-6, TNF-α, E-selectin, ICAM-1, and VCAM plasma levels.
Animal Model: Sprague-Dawley rats[1]
Dosage: 2 mg/kg
Administration: p.o. (Pharmacokinetic Analysis)
Result: The Cmax, dAUC and t1/2 were 1110 ng/mL, 6500 ng h/mL, and 4.25 hours, respectively.
Molecular Weight

446.43

Formula

C₂₁H₂₁F₃N₆O₂

CAS No.

752222-83-6

SMILES

O=C(N(CCC)C1=O)N(CC)C(C1=N2)=NC2C3=CN(N=C3)CC4=CC=CC(C(F)(F)F)=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >98.0%

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Keywords:

GS-6201CVT-6883GS6201GS 6201CVT6883CVT 6883Adenosine ReceptorP1 receptoraffinityselectivitycaspase-1cardiacremodelingacutemyocardialinfarctionairwayreactivityInhibitorinhibitorinhibit

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