周末想去喝酒

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“目录号: HY-15304

“目录号: HY-14813

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Cytoskeleton-

GPCR/G
Protein-

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Dynasore 是dynaminGTPase活性的抑制剂,IC50值为15 μM。

SA4503(AGY-94806; Cutamesine) is a selective sigma 1 receptor(σ1R)
agonist; high affinity for the sigma 1 receptor subtype labeled by
(+)-[3H]pentazocine (IC50 = 17.4 +/- 1.9 nM); 100-fold less affinity
for the sigma 2 receptor.

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Dynamin

Sigma
Receptor

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相关制品

连带产品

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Mdivi-1-

UNC0642-SA4503
dihydrochloride-Dextromethorphan
hydrobromide
hydrate-Noscapine-PRE-084
hydrochloride-S1RA
hydrochloride-4-IBP-BD-1047
dihydrobromide-Siramesine
hydrochloride-BD1063
dhydrochloride-Anavex
2-73-CYR-101-Dimemorfan
phosphate-Sigma-LIGAND-1-

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生物活性

生物活性

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Description

Description

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Dynasore is an inhibitor of the GTPase activity ofdynaminwith
anIC50of 15 μM.

SA4503(AGY-94806; Cutamesine) is a selective sigma 1 receptor(σ1R)
agonist; high affinity for the sigma 1 receptor subtype labeled by
(+)-[3H]pentazocine (IC50 = 17.4 +/- 1.9 nM); 100-fold less affinity
for the sigma 2 receptor.IC50 value: 17.4 nM [1]Target: σ1R agonistin
vitro: SA4503 showed little affinity for 36 other receptors, ion
channels and second messenger systems. SA4503 significantly increased
the KD value, but did not affect the Bmax value for specific
(+)-[3H]pentazocine binding. SA4503 is a potent and selective agonist
for the sigma 1 receptor subtype in the brain [1].  At concentrations
of 1-10μM, SA4503 reduced SOD1(G93A)-induced cell death in a
concentration-dependent manner [3].in vivo: The intravenous
administration of SA4503 (0.01-1.28 mg/kg) did not significantly alter
the firing rate or pattern of spontaneously active DA neurons in either
the SNC or VTA. A single injection of either 0.1 or 0.3 mg/kg i.p. of
SA4503 did not alter the number of spontaneously active SNC and VTA DA
neurons. In contrast, a single injection of 1 mg/kg i.p. of SA4503
produced a significant decrease and increase in the number of
spontaneously active SNC and VTA DA neurons, respectively[2]. SA4503
suppressed the progression of ALS in an SOD1(G93A) ALS mouse model.
SA4503 did not affect the onset time of ALS. However, it significantly
extended the survival time in the SOD1(G93A) mice compared with a
vehicle-treated group [3].

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