WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H531752
CAS#: 226948-11-4
Description: CRA1000 is a CRF1 receptor antagonist. CRA1000 is involved in the regulation of stress response.
Hodoodo Cat#: H531752
Name: CRA1000
CAS#: 226948-11-4
Chemical Formula: C28H33FN4S
Exact Mass: 476.24
Molecular Weight: 476.660
Elemental Analysis: C, 70.56; H, 6.98; F, 3.99; N, 11.75; S, 6.73
This product is not in stock, which may be available by custom synthesis.
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Synonym: CRA1000; CRA-1000; CRA 1000.
IUPAC/Chemical Name: N-ethyl-4-[4-(3-fluorophenyl)-3,6-dihydro-2H-pyridin-1-yl]-6-methyl-N-(2-methylsulfanyl-4-propan-2-ylphenyl)pyrimidin-2-amine
InChi Key: DDSMCPASYQDKFS-UHFFFAOYSA-N
InChi Code: InChI=1S/C28H33FN4S/c1-6-33(25-11-10-22(19(2)3)18-26(25)34-5)28-30-20(4)16-27(31-28)32-14-12-21(13-15-32)23-8-7-9-24(29)17-23/h7-12,16-19H,6,13-15H2,1-5H3
SMILES Code: CC(C1=CC=C(N(CC)C2=NC(C)=CC(N3CC=C(C4=CC=CC(F)=C4)CC3)=N2)C(SC)=C1)C
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 476.66 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: Knapp DJ, Overstreet DH, Moy SS, Breese GR. SB242084, flumazenil, and CRA1000 block ethanol withdrawal-induced anxiety in rats. Alcohol. 2004 Feb;32(2):101-11. PubMed PMID: 15163561; PubMed Central PMCID: PMC2871682.
2: Ohata H, Arai K, Shibasaki T. Effect of chronic administration of a CRF(1) receptor antagonist, CRA1000, on locomotor activity and endocrine responses to stress. Eur J Pharmacol. 2002 Dec 20;457(2-3):201-6. PubMed PMID: 12464367.
3: Chaki S, Okuyama S, Nakazato A, Kumagai T, Okubo T, Ikeda Y, Oshida Y, Hamajima Y, Tomisawa K. In vitro pharmacological profile of nonpeptide CRF1 receptor antagonists, CRA1000 and CRA1001. Eur J Pharmacol. 1999 Apr 29;371(2-3):205-11. PubMed PMID: 10357258.
4: Okuyama S, Chaki S, Kawashima N, Suzuki Y, Ogawa S, Nakazato A, Kumagai T, Okubo T, Tomisawa K. Receptor binding, behavioral, and electrophysiological profiles of nonpeptide corticotropin-releasing factor subtype 1 receptor antagonists CRA1000 and CRA1001. J Pharmacol Exp Ther. 1999 May;289(2):926-35. PubMed PMID: 10215672.
