SUN 1334H , CAS No.607736-84-5

Item Number
S649223
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S649223-1mg
1mg
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$94.90

Basic Description

Synonyms{4-[4-[Bis-(4-fluorophenyl)methyl]piperizin-1-yl]-(E)-but-2-enyloxy}acetic Acid Dihydrochloride | AKOS040739467 | SUN 1334H | SCHEMBL5623924 | CS-6696 | KAQMKGKFTBFMGE-SEPHDYHBSA-N | SCHEMBL1138186 | 2-[(E)-4-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]b
Biochemical and Physiological MechanismsSUN 1334H is a potent, orally active, highly selective H1 receptor antagonist, with K i of 9.7 nM.
Storage TempStore at 2-8°C,Desiccated
Shipped InWet ice
Product Description

SUN 1334H is a potent, orally active, highly selective H1 receptor antagonist, with K i of 9.7 nM.

In Vitro

SUN-1334H causes potent inhibition of histamine induced contractions of isolated guinea-pig ileum with an IC 50 (half the maximal inhibitory concentration) of 0.198 μM. In CHO-K1/hERG cells, SUN-1334H does not modulate hERG K + -currents at concentrations as high as 100 μM. SUN-1334H, cetirizine and hydroxyzine cause comparable inhibition of NLF leukocytes, IL-4 and total protein concentrations. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SUN-1334H potently inhibits histamine-induced bronchospasm over 24 hours following oral administration and completely suppresses histamine-induced skin wheal in beagle dogs and ovalbumin-induced rhinitis in guinea pigs . In skin allergy models, SUN-1334H shows potent reduction of passive and active cutaneous anaphylactic reactions. In central nervous system side effects models, SUN-1334H, desloratadine and fexofenadine are devoid of any significant effects. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:Ki: 9.7 nM (H1 receptor)

Names and Identifiers

IUPAC Name 2-[(E)-4-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]but-2-enoxy]acetic acid;dihydrochloride
INCHI InChI=1S/C23H26F2N2O3.2ClH/c24-20-7-3-18(4-8-20)23(19-5-9-21(25)10-6-19)27-14-12-26(13-15-27)11-1-2-16-30-17-22(28)29;;/h1-10,23H,11-17H2,(H,28,29);2*1H/b2-1+;;
InChi Key KAQMKGKFTBFMGE-SEPHDYHBSA-N
Canonical SMILES C1CN(CCN1CC=CCOCC(=O)O)C(C2=CC=C(C=C2)F)C3=CC=C(C=C3)F.Cl.Cl
Isomeric SMILES C1CN(CCN1C/C=C/COCC(=O)O)C(C2=CC=C(C=C2)F)C3=CC=C(C=C3)F.Cl.Cl
Alternate CAS 607736-84-5
PubChem CID 69509032
MeSH Entry Terms 4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-ylbut-2-enyloxy)acetic acid;SUN 1334H;SUN-1334H;SUN1334H
Molecular Weight 489.38

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