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509267 Sigma-AldrichOpn4 Antagonist - CAS 457961-34-1 - Calbiochem

Prevents melanopsin/Opn4 photoactivation in a reversible manner. Inhibits cellular phototransduction mediated by human Opn4 (IC₅₀ = 665 nM; using CHO transfectants).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

MSDS
参考
Data Sheet

同义词: Opn4 Antagonist, Opsinamide, Melanopsin-inhibiting Sulfonamide AA92593, Melanopsin Antagonist, Opsinamide AA92593, 1-(4-Methoxy-3-methyl-benzenesulfonyl)piperidine, 1-(4-Methoxy-3-methylphenylsulfonyl)piperidine

Primary Target: melanopsin (Opn4)

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概述

Replacement Information

重要规格表

CAS #	Empirical Formula
457961-34-1	C₁₃H₁₉NO₃S

价格及供货情况

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Description
Overview	A sulfonamide compound that prevents melanopsin/Opn4 photoactivation in a reversible and cis-Retinal-competitive manner without apparent affinity toward bovine retina rhodopsin or a panel of 74 other receptors, ion channels, and enzymes. Effectively inhibits cellular phototransduction mediated by human Opn4 (IC₅₀ = 665 nM; using CHO transfectants), murine Opn4 (IC₅₀ = 190 nM; using transfected Xenopus oocytes), and rat Opn4 (10 µM; using primary rat ipRGCs). Shown to effectively suppress PLR (pupillary light reflex; pupil constriction) in a time- and Opn4-dependent manner in mice (30 mg/kg i.p.) in vivo. Likewise, blue light insensitivity is observed in Opn4^-/- and AA92593-treated wild-type, but not vehicle-treated wild-type, P14 neonatal mice.
Catalogue Number	509267
Brand Family	Calbiochem®
Synonyms	Opn4 Antagonist, Opsinamide, Melanopsin-inhibiting Sulfonamide AA92593, Melanopsin Antagonist, Opsinamide AA92593, 1-(4-Methoxy-3-methyl-benzenesulfonyl)piperidine, 1-(4-Methoxy-3-methylphenylsulfonyl)piperidine

References
References	Jones, K.A., et al. 2013. Nat. Chem. Biol. 9, 630.

Product Information
CAS number	457961-34-1
Form	White solid
Hill Formula	C₁₃H₁₉NO₃S
Chemical formula	C₁₃H₁₉NO₃S
Reversible	Y
Structure formula Image
Quality Level	MQ100

Applications

Biological Information
Primary Target	melanopsin (Opn4)
Primary Target K<sub>i</sub>	110 and 160 nM for human and mouse melanopsin, respectively)
Purity	≥98% by HPLC

Physicochemical Information
Cell permeable	Y

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Ambient Temperature Only
Toxicity	Regulatory Review
Storage	+2°C to +8°C
Protect from Light	Protect from light
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 monthst at -20°C.

Packaging Information
Packaged under inert gas	Packaged under inert gas

Transport Information

Supplemental Information

Specifications

Global Trade Item Number
产品目录编号	GTIN
5.09267.0001	04055977241747

Documentation

Opn4 Antagonist - CAS 457961-34-1 - Calbiochem MSDS

职位
物料安全数据表 (MSDS)

参考

参考信息概述
Jones, K.A., et al. 2013. Nat. Chem. Biol. 9, 630.

数据表

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision	21-February-2014 JSW
Synonyms	Opn4 Antagonist, Opsinamide, Melanopsin-inhibiting Sulfonamide AA92593, Melanopsin Antagonist, Opsinamide AA92593, 1-(4-Methoxy-3-methyl-benzenesulfonyl)piperidine, 1-(4-Methoxy-3-methylphenylsulfonyl)piperidine
Description	A sulfonamide compound that prevents melanopsin/Opn4 photoactivation in a reversible and cis-Retinal-competitive manner (K_b = 6 and 0.16 µM in competitive binding studies using Opn4 pre-bound with cis-Retinal or not) without apparent affinity toward bovine retina rhodopsin or a panel of 74 other receptors, ion channels, and enzymes. Effectively inhibits cellular phototransduction mediated by human Opn4 in CHO transfectants (IC₅₀ = 665 nM; drug added 30 min before 10 µM 9-cis-Retinal & photoactivation), by murine Opn4 in transfected Xenopus oocytes (IC₅₀ = 190 nM; drug added 3 min before 50 µM 11-cis-Retinal and photoactivation), as well as by endogenous Opn4 in primary rat ipRGCs (intrinsically photosensitive retinal ganglion cells; 10 µM). Shown to be bioavailable in mice via i.p. injection (retina [AA92593] ~7.5 µM 30 min post 30 mg/kg i.p. dosing; >95% clearance within 2 h) and effectively suppress PLR (pupillary light reflex; pupil constriction) in a time- and Opn4-dependent manner in mice in vivo. Likewise, blue light insensitivity is observed in Opn4^-/- and AA92593-treated wild-type, but not vehicle-treated wild-type, P14 neonatal mice.
Form	White solid
Intert gas (Yes/No)	Packaged under inert gas
CAS number	457961-34-1
Chemical formula	C₁₃H₁₉NO₃S
Structure formula
Purity	≥98% by HPLC
Solubility	DMSO (100 mg/ml)
Storage	Protect from light +2°C to +8°C
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 monthst at -20°C.
Toxicity	Regulatory Review
References	Jones, K.A., et al. 2013. Nat. Chem. Biol. 9, 630.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > G-Protein and Related

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