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Description
Overview
A selective, high affinity , orally bioavailable 5-HT2B receptor antagonist. RS-127445 was found to have nanomolar affinity for the 5-HT2B receptor (pKi = 9.5) and 1,000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites including the closely related 5-HT2A and 5-HT2C receptors. In isolated human cells, RS-127445 exbhited an IC50 greater than 10 µM.
Catalogue Number
508147
Brand Family
Calbiochem®
References
References
Sharif, N. A. et al. 2006. J. Ocul. Pharmacol. Ther.22, 389. Bonhaus, D. W. et al. 1999. Br. J. Pharmacol.127, 1075. Bonhaus, D. W. et al. 1999. Br. J. Pharmacol.127, 1075.
Product Information
CAS number
199864-86-3
Form
Off-white solid
Hill Formula
C₁₇H₁₆FN₃·HCl
Chemical formula
C₁₇H₁₆FN₃·HCl
Structure formula Image
Applications
Biological Information
Primary Target
5-HT2B
Purity
≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code
Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity
Standard Handling
Storage
+2°C to +8°C
Protect from Light
Protect from light
Do not freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Transport Information
Supplemental Information
Specifications
Documentation
References
Reference overview
Sharif, N. A. et al. 2006. J. Ocul. Pharmacol. Ther.22, 389. Bonhaus, D. W. et al. 1999. Br. J. Pharmacol.127, 1075. Bonhaus, D. W. et al. 1999. Br. J. Pharmacol.127, 1075.
Data Sheet
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
25-October-2013 JSW
Description
A selective, high affinity , orally bioavailable 5-HT2B receptor antagonist. RS-127445 was found to have nanomolar affinity for the 5-HT2B receptor (pKi = 9.5) and 1,000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites including the closely related 5-HT2A and 5-HT2C receptors. In isolated human cells, RS-127445 exbhited an IC50 greater than 10 µM.
Form
Off-white solid
CAS number
199864-86-3
Chemical formula
C₁₇H₁₆FN₃·HCl
Structure formula
Purity
≥98% by HPLC
Solubility
DMSO (100 mM) or Ethanol (100 mM)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Sharif, N. A. et al. 2006. J. Ocul. Pharmacol. Ther.22, 389. Bonhaus, D. W. et al. 1999. Br. J. Pharmacol.127, 1075. Bonhaus, D. W. et al. 1999. Br. J. Pharmacol.127, 1075.