[CAS NO. 599179-03-0] Vicrivirocmaleate

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PRODUCTS SPECIFICATIONS [599179-03-0]

Catalog

HY-17377

Brand

MCE

CAS

599179-03-0

DESCRIPTION [599179-03-0]

Overview

MDL	MFCD09833218
Molecular Weight	649.70
Molecular Formula	C32H42F3N5O6
SMILES	CC1(N2C[C@H](C)N([C@H](C3=CC=C(C(F)(F)F)C=C3)COC)CC2)CCN(C(C4=C(C)N=CN=C4C)=O)CC1.O=C(O)/C=C\C(O)=O

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

Summary

Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5 , with a K _i of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC ₉₀ s of 3.3 nM (JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) and 10 nM (RU 570).

IC50 & Target

CCR5

2.5 nM (Ki)

HIV-1 (301657)

1.8 nM (IC90, in PBMC cells)

HIV-1 (ADA-M)

2.8 nM (IC90, in PBMC cells)

HIV-1 (JrFL)

3.3 nM (IC90, in PBMC cells)

HIV-1 (JV1083)

4.9 nM (IC90, in PBMC cells)

HIV-1 (RU 570)

10 nM (IC90, in PBMC cells)

In Vitro

Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective and oral bioavailable inhibitor of CCR5, with a K _i of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC ₉₀ s of 3.3 (JrFL), 2.8 (ADA-M), 1.8 (301657), 4.9 (JV1083) and 10 nM (RU 570). In addition, Vicriviroc maleate shows a mean IC ₅₀ and IC ₉₀ of 0.45 nM and 4 nM for a panel of HIV isolates, and has weak activity against hERG activity (IC ₅₀ , 5.8 μM) ^[1] . Vicriviroc maleate inhibits chemotactic response to MIP-1α with IC ₅₀ values below 1 nM, and suppresses RANTES-induced signaling with a mean IC ₅₀ of 4.2 ± 1.3 nM. Vicriviroc maleate potently suppresses all the viral isolates tested, with geometric mean EC ₅₀ s of 0.04-2.3 nM and IC ₉₀ s of 0.45-18 nM ^[2] .

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

In Vivo

Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate; 10 mg/kg) has good oral availablity in rats and monkeys, with no acute CNS or GI effects in rats ^[1] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00551018	Merck Sharp & Dohme LLC	HIV Infections	December 2007	Phase 2
NCT00766597	National Institute of Allergy and Infectious Diseases (NIAID)\|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)	HIV Infections	August 2009	Phase 1\|Phase 2
NCT00686829	Merck Sharp & Dohme LLC	HIV\|HIV Infections	June 30, 2005	Phase 2
NCT02356302	National Institute of Allergy and Infectious Diseases (NIAID)	HIV Infections	May 2015	Phase 1
NCT00243230	Merck Sharp & Dohme LLC	HIV Infections	September 19, 2005	Phase 2
NCT00632073	Merck Sharp & Dohme LLC	HIV Infections	March 2008	Phase 1
NCT00705419	Merck Sharp & Dohme LLC	HIV Infections	July 2007
NCT00551330	Merck Sharp & Dohme LLC	HIV Infections\|Acquired Immunodeficiency Syndrome	September 2007	Phase 2
NCT00474370	Merck Sharp & Dohme LLC	HIV Infections\|Acquired Immunodeficiency Syndrome	May 15, 2007	Phase 3
NCT00523211	Merck Sharp & Dohme LLC	HIV Infections\|Acquired Immunodeficiency Syndrome	July 2007	Phase 3
NCT00082498	National Institute of Allergy and Infectious Diseases (NIAID)\|AIDS Clinical Trials Group	HIV Infections	May 2004	Phase 2
NCT00243568	Merck Sharp & Dohme LLC	HIV Infections\|Acquired Immunodeficiency Syndrome	September 1, 2005	Phase 3
NCT03631407	Merck Sharp & Dohme LLC	Colorectal Neoplasms	September 24, 2018	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 76.96 mM ; Need ultrasonic)

H ₂ O : 25 mg/mL ( 38.48 mM ; Need ultrasonic and warming)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5392 mL	7.6959 mL	15.3917 mL
5 mM	0.3078 mL	1.5392 mL	3.0783 mL
10 mM	0.1539 mL	0.7696 mL	1.5392 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (3.85 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (3.85 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (3.85 mM); Clear solution

* All of the co-solvents are available by MCE.