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Nav1.7-IN-8 is a potent blockage of NaV1.7 with high selectivity for the inhibition of NaV1.7 over the subtypes hNaV1.1 and hNaV1.5. Nav1.7-IN-8 inhibits CYP2C9 and CYP3A4 with an IC50 of 0.17 μM and 0.077 μM, respectively. Nav1.7-IN-8 displays significant analgesic effects in rodent models of acute and inflammatory pain.
Product information
CAS Number: 1432913-44-4
Molecular Weight: 535.93
Formula: C21H12ClF2N5O4S2
Chemical Name: 4-[2-(3-amino-1,2-benzoxazol-5-yl)-4-chlorophenoxy]-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzene-1-sulfonamide
Smiles: NC1=NOC2=CC=C(C=C21)C1C=C(Cl)C=CC=1OC1=CC(F)=C(C=C1F)S(=O)(=O)NC1=NC=NS1
InChiKey: CYBITNCPJFQMIJ-UHFFFAOYSA-N
InChi: InChI=1S/C21H12ClF2N5O4S2/c22-11-2-4-16(12(6-11)10-1-3-17-13(5-10)20(25)28-33-17)32-18-7-15(24)19(8-14(18)23)35(30,31)29-21-26-9-27-34-21/h1-9H,(H2,25,28)(H,26,27,29)
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:
Nav1.7-IN-8 plasma protein binding is very high in rat with a free fraction of ∼1.1 %.
In Vivo:
Nav1.7-IN-8 (0~100 mpk, i.p.; 1 hour) shows a reduction of the pain response in phase 2a of the formalin assay in a dose dependent manner and produces a substantial inhibition of the pain response. . Nav1.7-IN-8 (10~100 mpk, i.p.; 2 days) displays a dose-dependent reduction of the pain response.
Products are for research use only. Not for human use.
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