Description
SUN 1334H is a potent, orally active, highly selective H1 receptor antagonist, with Ki of 9.7 nM.
Product information
CAS Number: 607736-84-5
Molecular Weight: 489.38
Formula: C23H28Cl2F2N2O3
Chemical Name: (E)-2-((4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)but-2-en-1-yl)oxy)acetic acid dihydrochloride
Smiles: Cl.Cl.OC(=O)COC/C=C/CN1CCN(CC1)C(C1C=CC(F)=CC=1)C1C=CC(F)=CC=1
InChiKey: KAQMKGKFTBFMGE-SEPHDYHBSA-N
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+;;
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
SUN-1334H causes potent inhibition of histamine induced contractions of isolated guinea-pig ileum with an IC50 (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.
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.
Products are for research use only. Not for human use.
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