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SB366791

SKU: orb1222227

Description

SB-366791is a potent and selective TRPV1 antagonist. SB-366791 inhibits glutamatergic synaptic transmission in rat spinal dorsal horn following peripheral inflammation. SB-366791 decreased capsaicin-induced Ca2+ influx in cultured trigeminal ganglion cells in a concentration-dependent manner (0.5-10 microM) with an IC50 of 651.9 nM. SB366791 is a more selective and in vivo also a more potent TRPV1 receptor antagonist than capsazepine in the rat therefore, it may promote the assessment of the therapeutic utility of TRPV1 channel blockers.

Images & Validation

Key Properties

CAS Number472981-92-3
MW287.74
Purity>98% (HPLC)
FormulaC16H14ClNO2
SMILESCOC1=CC=CC(=C1)NC(=O)/C=C/C2=CC=C(C=C2)Cl
TargetTRPV1
SolubilityDMSO : ≥ 39 mg/mL 135.54 mM; H2O : < 0.1 mg/mL

Bioactivity

In Vivo
SB-366791 (30 μM) inhibits the frequency of miniature excitatory postsynaptic currents (EPSCs). SB-366791 (30 μM) reduces the frequency of spontaneous EPSCs in the spinal cord slices from FCA-treated rats. SB-366791(30 μM) inhibits the amplitude of C-fibre evoked EPSCs. SB-366791 has also been used In vivo to assess the potential analgesic action of the inhibition of TRPV1, and significantly inhibits capsaicin-induced hypothermia, eye wiping movements and vasodilatation in the knee joint. SB-366791 inhibits glutamatergic transmission via an apparently pre-synaptic mechanism(s).

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

SB-366791 | SB 366791 | SB366791

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  • SB-366791 [orb1300295]

    >98%

    472981-92-3

    287.75

    C16H14ClNO2

    10 mg, 50 mg
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Protocol Information

SB366791 (orb1222227)

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Available Sizes

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200 mg
500 mg
2 mg
¥ 1,040.00
5 mg
¥ 1,170.00
10 mg
¥ 1,430.00
25 mg
¥ 2,730.00
50 mg
¥ 3,900.00
100 mg
¥ 6,240.00