BMS-582949 (hydrochloride)
- Product Name
- BMS-582949 (hydrochloride)
- CAS No.
- 912806-16-7
- Chemical Name
- BMS-582949 (hydrochloride)
- Synonyms
- BMS-582949 (hydrochloride);BMS-582949 hydrochloride, 10 mM in DMSO;BMS 582949,BMS 582949 hydrochloride,Inhibitor,BMS582949,Autophagy,BMS-582949,inhibit,BMS582949 hydrochloride,p38 MAPK;4-((5-(Cyclopropylcarbamoyl)-2-methylphenyl)amino)-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide hydrochloride
- CBNumber
- CB23126697
- Molecular Formula
- C22H27ClN6O2
- Formula Weight
- 442.94178
- MOL File
- 912806-16-7.mol
BMS-582949 (hydrochloride) Property
- storage temp.
- Store at -20°C
- solubility
- ≥44.3 mg/mL in DMSO with gentle warming; insoluble in H2O; ≥2.7 mg/mL in EtOH with gentle warming and ultrasonic
- form
- solid
- color
- White to off-white
Safety
- HS Code
- 2933998090
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- B7850
- Product name
- BMS-582949hydrochloride
- Packaging
- 5mg
- Price
- $150
- Updated
- 2021/12/16
- Product number
- CS-5621
- Product name
- BMS-582949hydrochloride
- Purity
- 98.82%
- Packaging
- 5mg
- Price
- $150
- Updated
- 2021/12/16
- Product number
- BISN0242
- Product name
- BMS-582949hydrochloride
- Packaging
- 5mg
- Price
- $203
- Updated
- 2021/12/16
- Product number
- CS-5621
- Product name
- BMS-582949hydrochloride
- Purity
- 98.82%
- Packaging
- 10mg
- Price
- $250
- Updated
- 2021/12/16
- Product number
- BISN0242
- Product name
- BMS-582949hydrochloride
- Packaging
- 10mg
- Price
- $363
- Updated
- 2021/12/16
BMS-582949 (hydrochloride) Chemical Properties,Usage,Production
Uses
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].
Biological Activity
bms-582949 hydrochloride is a novel, potent and highly selective p38α mitogen-activated protein kinase (p38α mapk) inhibitor [1].the p38α map kinase plays a critical role in regulating the production of many inflammatory cytokines, including tnf-α and il-1β. excessive production of tnf-α and il-1β has been implicated in many inflammatory diseases [1].bms-582949 hydrochloride potently inhibited the activity of p38α mapk with the ic50 value of 13 nm [1]. bms-582949 showed no significant effects on cytochrome p450 isozymes 1a2, 2c9, 2c19, and 2d6 with the ic50 values of >40 μm. bms-582949 weakly inhibited the activity of cyp3a4, with the ic50 value of 18-40 μm. bms-582949 displayed >2000-fold selectivity for p38α over a diverse panel of 57 kinases, include serine kinases, receptor tyrosine kinases, nonreceptor tyrosine kinases, and the p38γ and δ isoforms. bms-582949 showed 450-fold selectivity over jnk2, a map kinase involved in inflammation, and 190-fold selective over raf [1]. in mice, after oral administration of bms-582949 (10 mg/kg), the clearance rate for bms-582949 is 4.4 ml/min/kg. bms-582949 exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively [1].bms-582949 is currently under phase ii
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. |
IC 50
p38α MAPK: 13 nM (IC50); TNFα: 50 nM (IC50, in cells)
References
[1] liu c, lin j, wrobleski s t, et al. discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-n-propylpyrrolo [1, 2-f][1, 2, 4] triazine-6-carboxamide (bms-582949), a clinical p38α map kinase inhibitor for the treatment of inflammatory diseases[j]. journal of medicinal chemistry, 2010, 53(18): 6629-6639.
[2] emami h, vucic e, subramanian s, et al. the effect of bms-582949, a p38 mitogen-activated protein kinase (p38 mapk) inhibitor on arterial inflammation: a multicenter fdg-pet trial[j]. atherosclerosis, 2015, 240(2): 490-496.
BMS-582949 (hydrochloride) Preparation Products And Raw materials
Raw materials
Preparation Products
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