AMG 369 - CAS 1202073-26-4
Catalog number:
1202073-26-4
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C26H22FN3O2S
Molecular Weight:
459.54
COA:
Inquire
Targets:
Sphingosine 1 Phosphate Receptor
Description:
This active molecular is a S1P1/S1P5 agonist with limited activity at S1P3. AMG 369 has no activity at S1P2 and S1P4. AMG-369 is shown to reduce blood lymphocyte counts 24 hours postdose with dosed orally at 0.1 mg/kg. Till Jun 2016, no recent reports of development identified for preclinical development in Multiple-sclerosis in USA were published yet.
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Purity:
98%
Appearance:
Powder
Synonyms:
1-[[3-fluoro-4-[6-(1-phenylcyclopropyl)-[1,3]thiazolo[5,4-b]pyridin-2-yl]phenyl]methyl]azetidine-3-carboxylicacid;AMG369;ZINC216149127;KB-74649;1202073-26-4
Solubility:
Soluble in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
Multiple sclerosis
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
DSAOIEDPZKHAOM-UHFFFAOYSA-N
InChI:
InChI=1S/C26H22FN3O2S/c27-21-10-16(13-30-14-17(15-30)25(31)32)6-7-20(21)23-29-22-11-19(12-28-24(22)33-23)26(8-9-26)18-4-2-1-3-5-18/h1-7,10-12,17H,8-9,13-15H2,(H,31,32)
Canonical SMILES:
C1CC1(C2=CC=CC=C2)C3=CC4=C(N=C3)SC(=N4)C5=C(C=C(C=C5)CN6CC(C6)C(=O)O)F
Current Developer:
Amgen
1.Discovery of AMG 369, a Thiazolo[5,4-b]pyridine Agonist of S1P1 and S1P5.
Cee VJ1, Frohn M1, Lanman BA1, Golden J1, Muller K1, Neira S1, Pickrell A1, Arnett H2, Buys J1, Gore A1, Fiorino M1, Horner M1, Itano A1, Lee MR1, McElvain M1, Middleton S1, Schrag M1, Rivenzon-Segal D3, Vargas HM1, Xu H1, Xu Y1, Zhang X1, Siu J1, Wong M1 ACS Med Chem Lett. 2010 Dec 29;2(2):107-12. doi: 10.1021/ml100306h. eCollection 2011.
The optimization of a series of thiazolopyridine S1P1 agonists with limited activity at the S1P3 receptor is reported. These efforts resulted in the discovery of 1-(3-fluoro-4-(5-(1-phenylcyclopropyl)thiazolo-[5,4-b]pyridin-2-yl)benzyl)azetidine-3-carboxylic acid (5d, AMG 369), a potent dual S1P1/S1P5 agonist with limited activity at S1P3 and no activity at S1P2/S1P4. Dosed orally at 0.1 mg/kg, 5d is shown to reduce blood lymphocyte counts 24 h postdose and delay the onset and reduce the severity of experimental autoimmune encephalomyelitis in rat.
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CAS 1202073-26-4 AMG 369

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