Varenicline Tartrate

SKU: orb1225165

Description

Varenicline Tartrate is a nicotinic AChR partial agonist, used to treat nicotine addiction.

Images & Validation

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Key Properties

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CAS Number	375815-87-5
MW	361.35
Purity	>98% (HPLC)
Formula	C₁₃H₁₃N₃·C₄H₆O₆
SMILES	C1[C@@H]2CNC[C@H]1C3=CC4=NC=CN=C4C=C23.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O
Target	AChR
Solubility	Water: 72 mg/mL (199.25 mM); DMSO: 1 mg/mL (2.76 mM)

Bioactivity

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In Vitro

Cell Viability Assay Cell line: HUVEC. Concentration: 100, 200, 300, 500 μM. Incubation time: 24 h. Result: Did not affect cell viability at 100 and 200 μM (96.8 ± 0.1% and 93.9 ± 1.8%, respectively). Decreased cell viability to 85.7 ± 7.5% and 57.8 ± 7.7% for 300 and 500 μM, respectively. Western blot analysis. Cell line: HUVEC. Concentration: 100 μM. Incubation time: 1, 5, 10, 15, 30, 60 min, 24 h. Result: Significantly activated ERK1/2 and p38 signaling with peak activity at 10-15 min and 10-30 min after treatment, respectively, lowered expression of VE-cadherin at 24 h. MLA (100 nM) significantly reversed the Varenicline-induced effects. Cell Migration Assay Cell line: HUVEC. Concentration: 100 μM. Incubation time: 4 h. Result: Significantly increased the number of migrating cells by 2.4-fold compared with vehicle treatment. MLA (100 nM) completely blocked Varenicline-stimulated migration.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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CP 526,555-18

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Gene Symbol

AChR

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