1. Membrane Transporter/Ion Channel
  2. P2X Receptor
  3. GW791343 dihydrochloride

GW791343 dihydrochloride 

Cat. No.: HY-15469
Handling Instructions

GW791343 2Hcl is a P2X7 allosteric modulator; exhibits species-specific activity and acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2).

For research use only. We do not sell to patients.

GW791343 dihydrochloride Chemical Structure

GW791343 dihydrochloride Chemical Structure

CAS No. : 1019779-04-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 456 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
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Other Forms of GW791343 dihydrochloride:

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Description

GW791343 2Hcl is a P2X7 allosteric modulator; exhibits species-specific activity and acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2). IC50 value: 7 (pIC50) Target: P2X7 in vitro: In cells expressing human P2X7 receptors, GW 791343 inhibits agonist-stimulated ethidium accumulation in both sucrose and NaCl buffer. In NaCl buffer, GW 791343 reduces the maximal response to both ATP and BzATP, but there is little effect on agonist potency except for a decrease in the presence of 300–1000 nM GW 791343. GW 791343 also reduces maximal responses to ATP and BzATP in sucrose buffer, although this effect is more marked when using ATP as agonist. In sucrose buffer, GW 791343 produces a slight decrease in ATP potency at 300 nM. GW 791343 decreases BzATP potency at concentrations of 300 nM to 10 μM. A more marked increase in agonist effect is observed when using ATP as agonist in NaCl buffer with GW791343 increasing the pEC50 and maximal response to ATP at concentrations of 10 and 30 μM. In sucrose buffer, GW791343 also increases responses when using ATP as agonist [1]. GW791343 inhibits responses at the human–rat chimeric receptor in both sucrose and NaCl buffer. GW791343 increases responses to BzATP at the F95L mutant receptor [2]. GW791343 is a non-competitive antagonist and negative allosteric modulator at the human P2X7 receptor; however, GW 791343 also acts as a positive allosteric modulator at the rat P2X7 receptor [3]. At the dog P2X7 receptor, GW 791343 is an antagonist with similar potency to that determined at the human receptor [4].

Storage

4°C, stored under nitrogen

Solvent & Solubility
In Vitro: 

DMSO : ≥ 42 mg/mL (93.89 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2354 mL 11.1769 mL 22.3539 mL
5 mM 0.4471 mL 2.2354 mL 4.4708 mL
10 mM 0.2235 mL 1.1177 mL 2.2354 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

447.35

Formula

C₂₀H₂₆Cl₂F₂N₄O

CAS No.

1019779-04-4

SMILES

O=C(NC1=CC(CN2CCNCC2)=CC=C1C)CNC3=CC=C(F)C(F)=C3.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
GW791343 dihydrochloride
Cat. No.:
HY-15469
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GW791343 dihydrochloride

Cat. No.: HY-15469