WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H530966
CAS#: 1420071-13-1
Description: LAS191859 is a CRTH2/DP2 antagonist with IC50 values of 9.58, 14, 15.5, and 7.6 nM for recombinant human, rat, mouse, and guinea pig CRTH2/DP2 receptors, respectively. In vitro evidence in GTPγS binding studies indicate that LAS191859 is a CRTh2 antagonist with activity in the low nanomolar range. This potency is also maintained in cellular assays performed with human eosinophils and whole blood. The main differentiation of LAS191859 vs other CRTh2 antagonists is in its receptor binding kinetics. LAS191859 has a residence time half-life of 21h at CRTh2 that translates into a long-lasting in vivo efficacy that is independent of plasma levels
Hodoodo Cat#: H530966
Name: LAS191859
CAS#: 1420071-13-1
Chemical Formula: C24H24F3N3O3
Exact Mass: 459.18
Molecular Weight: 459.469
Elemental Analysis: C, 62.74; H, 5.27; F, 12.40; N, 9.15; O, 10.45
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Synonym: LAS191859; LAS-191859; LAS 191859.
IUPAC/Chemical Name: 2-(1-(2-((N-ethylcyclopropanecarboxamido)methyl)-4-(trifluoromethyl)phenyl)-6-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)acetic acid
InChi Key: KGBYKYDRYYERIX-UHFFFAOYSA-N
InChi Code: InChI=1S/C24H24F3N3O3/c1-3-29(23(33)15-5-6-15)12-17-10-18(24(25,26)27)7-9-20(17)30-13-16(11-21(31)32)19-8-4-14(2)28-22(19)30/h4,7-10,13,15H,3,5-6,11-12H2,1-2H3,(H,31,32)
SMILES Code: CCN(CC1=CC(C(F)(F)F)=CC=C1N2C=C(C3=C2N=C(C=C3)C)CC(O)=O)C(C4CC4)=O
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
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 459.47 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: Calbet M, Andrés M, Armengol C, Bravo M, Eichhorn P, López R, García-González
V, Roberts R, Miralpeix M. Pharmacological characterization of CRTh2 antagonist
LAS191859: Long receptor residence time translates into long-lasting in vivo
efficacy. Pharmacol Res. 2016 Sep;111:208-216. doi: 10.1016/j.phrs.2016.06.014.
Epub 2016 Jun 16. PubMed PMID: 27317944.