1. Anti-infection
    Metabolic Enzyme/Protease
  2. HIV
    HIV Integrase
  3. GSK3739936

GSK3739936 (Synonyms: BMS-986180)

Cat. No.: HY-150080
Handling Instructions

GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability.

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

GSK3739936 Chemical Structure

GSK3739936 Chemical Structure

CAS No. : 1803444-21-4

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Description

GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability[1].

IC50 & Target

IC50: 11.1 nM (HIV-1 integrase)[1]
EC50: 1.7 nM (HIV-1 integrase)[1]
IC50: >24.3 μM (CYP)[1]

In Vitro

GSK3739936 is not cytotoxic to MT-2 cells, exhibiting CC50 values of >20 μM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GSK3739936 exhibits favorable pharmacokinetic property with rapid absorption, low to moderate clearance and excellent oral bioavailability[1].
Pharmacokinetic Parameters of GSK3739936 in Preclinical Species[1].

Male CD-1 mice Male Sprague-Dawley rats Cynomolgus monkey Male beagle dogs
IV dose (mg/kg) 1 1 1 1
CL (mL/min/kg) 5.4 5.5 14.5 2.9
t1/2 (h) 6.3 4.3 2.4 5.1
Vss (L/kg) 2.4 1.8 1.5 0.7
PO dose (mg/kg) 5 5 2 2
Cmax (nM) 2361 2762 525 2963
tmax (h) 5 2.7 2 2
AUC (nM·h) 24516 14022 2231 18471
F (%) 89 52 54 75

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male CD-1 mice, male Sprague-Dawley rats, cynomolgus monkey and male beagle dogs[1]
Dosage: 1 mg/kg for IV; 5 or 2 mg/kg for PO
Administration: PO or IV; single dosage
Result: Exhibited a low clearance in the mouse, rat, and dog with moderate to long elimination half-lives, while displays moderate clearance and a short elimination half-life in the cynomolgus monkey.
The absolute oral bioavailability ranged between 52 and 89%.
The tmax value of 2-5 h suggesting rapid absorption in all four species.
Molecular Weight

562.71

Formula

C34H43FN2O4

CAS No.
SMILES

CC1=NC(C)=C(C(N2CCC(C)(CC2)C)=C1[[email protected]@H](C(O)=O)OC(C)(C)C)C3=CC=C(C=C3)OCCC4=CC=C(C=C4)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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GSK3739936
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