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MilliporeSigma

SML4292

SAF312

≥98% (HPLC), powder, TRPV1 antagonist

Synonym(s):

4-[7-Hydroxy-2-(1-methylethyl)-4-oxo-3(4H)-quinazolinyl]benzonitrile, 4-(7-Hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)benzonitril, Libvatrep, Vanilloid receptor antagonist 1

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About This Item

Empirical Formula (Hill Notation):
C18H15N3O2
CAS Number:
Molecular Weight:
305.33
NACRES:
NA.21
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

General description

SAF312 (Libvatrep), a quinazolinone derivative, is a potent and highly selective noncompetitive antagonist TRPV1 (transient receptor potential vanilloid 1) (IC50 = 14 nM).

Application

SAF312 may be used to evaluate the effects of its inhibitory action in CHO cells expressing human TRPV1.

Biochem/physiol Actions

SAF312 is a non-narcotic analgesic that is currently investigated as a treatment for ocular surface pain. SAF312 binds to the vanilloid binding pocket of TRPV1, which is located between the S3 and S4 helices of one subunit and the S5 and S6 domains of the adjacent subunit. This binding prevents crucial conformational changes in the S4 and S5 helices that are essential for channel gating.


pictograms

Exclamation mark

signalword

Warning

Hazard Classifications

Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2

Storage Class

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable



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