1. Membrane Transporter/Ion Channel
  2. Calcium Channel

Fantofarone (Synonyms: SR 33557)

Cat. No.: HY-105117 Purity: 98.56%
Handling Instructions

Fantofarone is a highly potent Calcium Channel antagonist.

For research use only. We do not sell to patients.

Fantofarone Chemical Structure

Fantofarone Chemical Structure

CAS No. : 114432-13-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 182 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 240 In-stock
Estimated Time of Arrival: December 31
50 mg USD 750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Fantofarone is a highly potent Calcium Channel antagonist.

IC50 & Target

Calcium Channel[1].

In Vitro

It can be seen that the calcium channel blockers VIZ and Fantofarone (SR) possess a weak intrinsic antimalarial property compared to CQ, and both appear slightly more potent on the CQ-resistant than on the CQ-sensitive parasites. Interestingly, Fantofarone is ca. 10 times more potent than verapamil. Fantofarone (SR) is 10 times more potent than the phenylalkylamine verapamil (VR) on the two P. fdciparum strains. As revealed by the isobolograms, the two calcium channel blockers potentiate the CQ sensitivity activity on the CQ-resistant P. fufcipurum strain, verapamil appearing 2 to 3 times more potent than Fantofarone. Furthermore, when used at similar subinhibitory fractions of their IC50, VR is 2 to 3 times more potent than Fantofarone in decreasing CQ resistance[1].

In Vivo

Treatment with isosorbide dinitrate (0.3 mg/kg, i.v.) or Fantofarone (50 mg/kg, i.v.), a reduction is observed in the occurrence and severity of vasospasm, whereas verapamil (0.2 mg/kg, i.v.) is much less effective. Although it totally inhibits distal AIV, isosorbide dinitrate does not significantly affect proximal diameter decrease. The most potent compound with regard to both the distal and proximal vasospasms is Fantofarone, which significantly reduces AIV throughout the experiment. Verapamil does not reduce AIV significantly[2].

Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (272.38 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8158 mL 9.0792 mL 18.1584 mL
5 mM 0.3632 mL 1.8158 mL 3.6317 mL
10 mM 0.1816 mL 0.9079 mL 1.8158 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[2]

Rabbits[2]
Male White rabbits are used in this study (3.0-3.2 kg). All surgical procedures are performed under anaesthesia with a mixture of ketamine and xylazine. At the end of the experiments, the animals are sacrificed by a pentobarbital overdose. The proximal femoral arteries are exposed, and the isolated arterial segments are desiccated by air infusion delivered at a rate of 80 mL/min for 8 min. After desiccation is completed, the ligatures are released and flow is restored. At the day of surgery, a 2% cholesterol/6% peanut oil diet is started for 2 weeks. Before angioplasty, the animals are randomized in 4 groups of 10 animals:1. Placebo, 1 mL/kg of NaCl 0.9%, 2. Isosorbide dinitrate, 0.3 mg/kg, 3. Verapamil, 0.2 mg/kg, 4. Fantofarone, 50 mg/kg. The doses of isosorbide dinitrate, verapamil, and fantofarone are defined in a pilot experiment as the highest doses which did not show any hypotensive effect per se and are chosen very carefully according to their activity measured in other pharmacological models[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

550.71

Formula

C₃₁H₃₈N₂O₅S

CAS No.

114432-13-2

SMILES

O=S(C1=C2N(C=CC=C2)C=C1C(C)C)(C3=CC=C(OCCCN(C)CCC4=CC(OC)=C(OC)C=C4)C=C3)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Fantofarone
Cat. No.:
HY-105117
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Fantofarone

Cat. No.: HY-105117