Clemastine fumarateA selective histamine H1 antagonist

Clemastine fumarate (CAS 14976-57-9)

Clemastine fumarate | CAS 14976-57-9 is rated 5.0 out of 5 by 1.
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Application: A selective histamine H1 antagonist
CAS Number: 14976-57-9
Purity: ≥98%
Molecular Weight: 459.97
Molecular Formula: C21H26ClNO C4H4O4
* Refer to Certificate of Analysis for lot specific data (including water content).
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Clemastine fumarate is a selective histamine H1 Receptor antagonist with IC50 of 3 nM. Clemastine Fumarate inhibits histamine induced rise in [Ca2+]i in HL-60 cells with an IC50 of 3 nM. Clemastine Fumarate significantly potentiates ATP-induced increase in [Ca2+]i in HEKhP2X7 cells not relying on histamine receptor blockage but on sensitizing P2X7 receptor.


References

1. Thomas, J.S., et al. 1977. Ann Allergy. 38: 169-174. PMID: 320916
2. Dockhorn, R.J., et al. 1982. Mo Med. 79: 748-750. PMID: 7177096
3. Nair, M.P., et al. 1983. Cell. Immunol. 81: 45-60. PMID: 6225527

Appearance :
Crystalline
Physical State :
Solid
Solubility :
Soluble in water (5 mM), methanol, DMSO (35 mg/ml), ethanol (3 mg/ml), and alcohol (slightly).
Storage :
Store at room temperature
Melting Point :
177-178° C (dec.)
Boiling Point :
154° C at 0.02 mmHg
Refractive Index :
n20D 1.55 (Predicted)
Optical Activity :
α20/D +20°±5°, c = 1 in methanol
IC50 :
Histamine H1 receptor: IC50 = 3 nM; histamine induced rise in [Ca2+]i : IC50 = 3 nM (HL-60 cells); histamine-induced contraction : IC50 = 0.23 µM (guinea pig ileum); Plasmodium falciparum: IC50 = 0.46 µM; Plasmodium berghei: IC50 = 0.95 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
RTECS :
UY0704600
PubChem CID :
5281069
MDL Number :
MFCD00137486
EC Number :
239-055-2
Beilstein Registry :
6472482
SMILES :
C[C@@](C1=CC=CC=C1)(C2=CC=C(C=C2)Cl)OCC[C@H]3CCCN3C.C(=C/C(=O)O)\\C(=O)O

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Ridley JM; et al Ridley JM; et al. (PubMed ID: 16288909) determined that Clemastine fumarate is a potent inhibitor of Human ether- -go-go-related gene and has a high affinity for HERG channel pore cavity. -SCBT Publication Review
Date published: 2015-05-16
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