Tetrandrine

SKU: orb1224830

Description

Tetrandrine (NSC 77037;Fanchinine) is a bis-benzylisoquinoline alkaloid that acts a calcium channel blocker (IC50= 8 and 20 uM for L-type and T-type calcium channels, respectively) and induces apoptosis; produces anti-inflammatory, immunomodulating, anti-proliferative, and free radical scavenging effects; has also been shown to increase glucose utilization by enhancing hepatocyte glycogen synthesis; a potent cell autophagy agonist.Lung Cancer Phase 3 Clinical(In Vitro):The effects of Tetrandrine (NSC-77037), a bis-benzyl-isoquinoline alkaloid, on voltage-gated Ca2+ currents (ICa) and on Ca2+-activated K+ current (IK(Ca)) and channels in isolated nerve terminals of the rat neurohypophysis are investigated using patch-clamp techniques. The non-inactivating component of ICa is inhibited by external Tetrandrine (NSC-77037) in a voltage- and dose-dependent manner, with an IC50=10.1μM. Tetrandrine (NSC-77037) decreases the channel-open probability, within bursts, with an IC50=0.21 μM. To evaluate the effects of Tetrandrine on HCC cells, Huh7, HCCLM9 and Hep3B cells are treated with 0 (DMSO), 0.5, 1, 2 or 4 μM of Tetrandrine for 24 h. The cell proliferation assay indicates that Tetrandrine exhibits almost no effect on the inhibition of HCC cell proliferation at 0.5-2 μM. However, Tetrandrine (NSC-77037) inhibits HCC cell migration in a dose-dependent manner. Furthermore, a wound-healing and transwell assay shows that 2 μM Tetrandrine significantly inhibits HCC cell migration and invasion.(In Vivo):To evaluate the effect of Tetrandrine (NSC-77037) on the inhibition of tumor metastasis in vivo, HCCLM9 subcutaneous tumor xenograft models is established with athymic nude mice. When the tumor volume reach approximately 50 mm3, nude mice are orally administered vehicle or Tetrandrine (NSC-77037) (30 mg/kg) every other day for 37 days. Tetrandrine (NSC-77037) treatment inhibits tumor growth by reducing the tumor volume and weight.

Key Properties

• CAS Number: 518-34-3
• MW: 622.8
• Purity: >98% (HPLC)
• Formula: C₃₈H₄₂N₂O₆
• SMILES: COC1=C(C2=C(C=C1OC)CCN(C)[C@]2(C3)[H])OC4=CC5=C(C=C4OC)CCN(C)[C@]5(CC6=CC=C(OC7=CC3=CC=C7OC)C=C6)[H]
• Target: Calcium Channel
• Solubility: DMSO: 1 mg/mL (1.61 mM); Ethanol: 2 mg/mL (3.21 mM), warmed; Water: <1 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vivo:
  To evaluate the effect of Tetrandrine (NSC-77037) on the inhibition of tumor metastasis In vivo, HCCLM9 subcutaneous tumor xenograft models is established with athymic nude mice. When the tumor volume reach approximately 50 mm3, nude mice are orally administered vehicle or Tetrandrine (NSC-77037) (30 mg/kg) every other day for 37 days. Tetrandrine (NSC-77037) treatment inhibits tumor growth by reducing the tumor volume and weight.
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• In Vitro:
  The effects of Tetrandrine (NSC-77037), a bis-benzyl-isoquinoline alkaloid, on voltage-gated Ca2+ currents (ICa) and on Ca2+-activated K+ current (IK(Ca)) and channels in isolated nerve terminals of the rat neurohypophysis are investigated using patch-clamp techniques. The non-inactivating component of ICa is inhibited by external Tetrandrine (NSC-77037) in a voltage- and dose-dependent manner, with an IC50 = 10.1 μM. Tetrandrine (NSC-77037) decreases the channel-open probability, within bursts, with an IC50 = 0.21 μM. To evaluate the effects of Tetrandrine on HCC cells, Huh7, HCCLM9 and Hep3B cells are treated with 0 (DMSO), 0.5, 1, 2 or 4 μM of Tetrandrine for 24 h. The cell proliferation assay indicates that Tetrandrine exhibits almost no effect on the inhibition of HCC cell proliferation at 0.5-2 μM. However, Tetrandrine (NSC-77037) inhibits HCC cell migration in a dose-dependent manner. Furthermore, a wound-healing and transwell assay shows that 2 μM Tetrandrine significantly inhibits HCC cell migration and invasion.
  Read more...

Storage & Handling

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

Alternative Names

NSC 77037 | Fanchinine

Quick Database Links

Gene Symbol

Calcium Channel