1. Membrane Transporter/Ion Channel Neuronal Signaling Anti-infection
  2. Calcium Channel Parasite
  3. Fantofarone

Fantofarone is a highly potent Calcium Channel antagonist.

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Fantofarone

Fantofarone 화학구조

CAS No. : 114432-13-2

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 1 publication(s) in Google Scholar

Other Forms of Fantofarone:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Fantofarone

  • Biological Activity

  • Protocol

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

Fantofarone is a highly potent Calcium Channel antagonist.

IC50 & Target

Calcium Channel[1].

Cellular Effect
Cell Line Type Value Description References
Ventricular myocyte IC50
0.022 3
Compound: SR33557 (fantofarone)
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
[PMID: 22761000]
P388/ADR IC50
30 3
Compound: 107; SR33557
Reversal of ABCB1 mediated doxorubicin-resistance in mouse P388/ADR cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Reversal of ABCB1 mediated doxorubicin-resistance in mouse P388/ADR cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
[PMID: 35751979]
P388/ADR IC50
30 3
Compound: 107; SR33557
Reversal of ABCB1 mediated doxorubicin-resistance in mouse P388/ADR cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Reversal of ABCB1 mediated doxorubicin-resistance in mouse P388/ADR cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
[PMID: 35751979]
Ventricular myocyte IC50
0.022 3
Compound: SR33557 (fantofarone)
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
[PMID: 22761000]
Ventricular myocyte IC50
9 3
Compound: SR33557 (fantofarone)
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
[PMID: 22761000]
Ventricular myocyte IC50
0.022 3
Compound: SR33557 (fantofarone)
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
[PMID: 22761000]
Ventricular myocyte IC50
9 3
Compound: SR33557 (fantofarone)
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
[PMID: 22761000]
Ventricular myocyte IC50
9 3
Compound: SR33557 (fantofarone)
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
[PMID: 22761000]
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].

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

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].

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

분자량

550.71

화학식

C31H38N2O5S

CAS No.
Appearance

Solid

Color

Light yellow to yellow

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

선적

Room temperature in continental US; may vary elsewhere.

보관
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
용액&용해도
In Vitro: 

DMSO : 100 mg/mL (181.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 몰농도 계산기

  • 농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.54 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.54 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서

Purity: 99.91%

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 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8158 mL 9.0792 mL 18.1584 mL 45.3959 mL
5 mM 0.3632 mL 1.8158 mL 3.6317 mL 9.0792 mL
10 mM 0.1816 mL 0.9079 mL 1.8158 mL 4.5396 mL
15 mM 0.1211 mL 0.6053 mL 1.2106 mL 3.0264 mL
20 mM 0.0908 mL 0.4540 mL 0.9079 mL 2.2698 mL
25 mM 0.0726 mL 0.3632 mL 0.7263 mL 1.8158 mL
30 mM 0.0605 mL 0.3026 mL 0.6053 mL 1.5132 mL
40 mM 0.0454 mL 0.2270 mL 0.4540 mL 1.1349 mL
50 mM 0.0363 mL 0.1816 mL 0.3632 mL 0.9079 mL
60 mM 0.0303 mL 0.1513 mL 0.3026 mL 0.7566 mL
80 mM 0.0227 mL 0.1135 mL 0.2270 mL 0.5674 mL
100 mM 0.0182 mL 0.0908 mL 0.1816 mL 0.4540 mL
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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상품명:
Fantofarone
Cat. No.:
HY-105117
수량:
MCE Japan Authorized Agent: