Description
Wy 49051 is a potent, orally active H1 receptor antagonist, with IC50 of 44 nM.
Product information
CAS Number: 113418-56-7
Molecular Weight: 487.59
Formula: C28H33N5O3
Chemical Name: 7-{3-[4-(diphenylmethoxy)piperidin-1-yl]propyl}-1,3-dimethyl-2,3,6,7-tetrahydro-1H-purine-2,6-dione
Smiles: CN1C(=O)C2=C(N=CN2CCCN2CCC(CC2)OC(C2C=CC=CC=2)C2C=CC=CC=2)N(C)C1=O
InChiKey: YNDYDETWRDHMLW-UHFFFAOYSA-N
InChi: InChI=1S/C28H33N5O3/c1-30-26-24(27(34)31(2)28(30)35)33(20-29-26)17-9-16-32-18-14-23(15-19-32)36-25(21-10-5-3-6-11-21)22-12-7-4-8-13-22/h3-8,10-13,20,23,25H,9,14-19H2,1-2H3
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:
Wy 49051 shows great inhibitory effect on H1, producing 92% inhibition of the histamine-induced contraction of the guinea pig ileum at a concentration 100 nM. Wy 49051 is the most potent compound with 700 times the potency of astemazole, 470 times the potency of chlorpheniramine. Wy 49051 also has high affinity for α1 receptor with IC50 of 8 nM.
In Vivo:
Wy 49051 shows potent activity against histamine-induced lethality in the guinea pig, with ED50 of 1.91 mg/kg by po, 0.70 mg/kg by ip, and 0.01 mg/kg by iv. The duration of action of 24 is also favorable since there is no decrease in oral efficacy up to 18 h posttreatment.
Products are for research use only. Not for human use.
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