1. MAPK/ERK Pathway
    Autophagy
  2. p38 MAPK
    Autophagy
  3. BMS-582949 hydrochloride

BMS-582949 hydrochloride 

Cat. No.: HY-14305A Purity: 98.82%
Handling Instructions

BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC50 of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease.

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

BMS-582949 hydrochloride Chemical Structure

BMS-582949 hydrochloride Chemical Structure

CAS No. : 912806-16-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 146 In-stock
Estimated Time of Arrival: December 31
1 mg USD 70 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
25 mg USD 500 In-stock
Estimated Time of Arrival: December 31
50 mg USD 750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1200 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

BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC50 of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease[1].

IC50 & Target

p38α MAPK

13 nM (IC50)

TNFα

50 nM (IC50, in cells)

In Vitro

BMS-582949 displays a p38α IC50 of 13 nM and a cellular TNFα IC50 of 50 nM[1].
BMS-582949 is a weak inhibitor of CYP3A4 BMS-582949 displays >2000-fold selectivity for p38α over a diverse panel of 57 kinases that include serine kinases, nonreceptor tyrosine kinases, receptor tyrosine kinases, and the p38γ and δ isoforms[1].

In Vivo

BMS-582949 (5-100 mg/kg, orally) is effective in both the acute murine model of inflammation and rat adjuvant arthritis model despite its slightly reduced potency[1].

Animal Model: Male Sprague-Dawley rats (250-300 g) adjuvant arthritis model[1].
Dosage: 1, 10, 100 mg/kg.
Administration: Orally once daily (from day 11 to day 19).
Result: Displayed dose-dependent reduction in paw swelling with qd dosing, with efficacy observed at doses of 10 and 100 mg/kg.
Clinical Trial
Molecular Weight

442.94

Formula

C₂₂H₂₇ClN₆O₂

CAS No.

912806-16-7

SMILES

O=C(NCCC)C1=CN(N=CN=C2NC3=CC(C(NC4CC4)=O)=CC=C3C)C2=C1C.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 35 mg/mL (79.02 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2576 mL 11.2882 mL 22.5764 mL
5 mM 0.4515 mL 2.2576 mL 4.5153 mL
10 mM 0.2258 mL 1.1288 mL 2.2576 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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BMS-582949 hydrochloride
Cat. No.:
HY-14305A
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