WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H524206
CAS#: 864249-60-5
Description: AMG-548 is a potent and selective inhibitor of p38α. It displays >1000-fold selectivity against 36 other kinases, and it inhibits whole blood LPS-stimulated TNFα. AMG-548 has shown to be efficacious in acute and chronic models of arthritis.
Hodoodo Cat#: H524206
Name: AMG 548
CAS#: 864249-60-5
Chemical Formula: C29H27N5O
Exact Mass: 461.22
Molecular Weight: 461.560
Elemental Analysis: C, 75.46; H, 5.90; N, 15.17; O, 3.47
Synonym: AMG 548; AMG-548; AMG548; UNII-PGR0H531I4;
IUPAC/Chemical Name: 4(3H)-Pyrimidinone, 2-(((2S)-2-amino-3-phenylpropyl)amino)-3-methyl-5-(2-naphthalenyl)-6-(4-pyridinyl)-
InChi Key: RQVKVJIRFKVPBF-VWLOTQADSA-N
InChi Code: InChI=1S/C29H27N5O/c1-34-28(35)26(24-12-11-21-9-5-6-10-23(21)18-24)27(22-13-15-31-16-14-22)33-29(34)32-19-25(30)17-20-7-3-2-4-8-20/h2-16,18,25H,17,19,30H2,1H3,(H,32,33)/t25-/m0/s1
SMILES Code: Cn1c(=O)c(c(nc1NC[C@H](Cc2ccccc2)N)c3ccncc3)c4ccc5ccccc5c4
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 461.56 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Verkaar F, van der Doelen AA, Smits JF, Blankesteijn WM, Zaman GJ. Inhibition of Wnt/β-catenin signaling by p38 MAP kinase inhibitors is explained by cross-reactivity with casein kinase Iδ/ɛ. Chem Biol. 2011 Apr 22;18(4):485-94. doi: 10.1016/j.chembiol.2011.01.015. PubMed PMID: 21513885.
2: Shields CJ, Delaney CP, Winter DC, Young L, Gorey TF, Fitzpatrick JM. Induction of nitric oxide synthase is a key determinant of progression to pulmonary injury in experimental pancreatitis. Surg Infect (Larchmt). 2006 Dec;7(6):501-11. PubMed PMID: 17233567.
3: Lee MR, Dominguez C. MAP kinase p38 inhibitors: clinical results and an intimate look at their interactions with p38alpha protein. Curr Med Chem. 2005;12(25):2979-94. Review. PubMed PMID: 16378500.
4: Owczuk R, Sawicka W, Wujtewicz MA, Kawecka A, Lasek J, Wujtewicz M. Influence of spinal anesthesia on corrected QT interval. Reg Anesth Pain Med. 2005 Nov-Dec;30(6):548-52. PubMed PMID: 16326340.
5: Dominguez C, Powers DA, Tamayo N. p38 MAP kinase inhibitors: many are made, but few are chosen. Curr Opin Drug Discov Devel. 2005 Jul;8(4):421-30. Review. PubMed PMID: 16022178.