Suvecaltamide (Synonyms: MK-8998; CX-8998; JZP385)

Name: Suvecaltamide
Brand: MedChemExpress
SKU: HY-101096
Rating: 4.5 (1 reviews)

Cat. No.: HY-101096 Purity: 99.96%: FAQs
Data Sheet SDS COA Handling Instructions

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Suvecaltamide (MK-8998) is a selective T-type calcium channel inhibitor with oral efficacy. Suvecaltamide exhibits no cytotoxicity in myeloma cell lines and does not affect the antitumor efficacy of Bortezomib (BTZ). Suvecaltamide reverses BTZ-induced peripheral neuropathy (CIPN) in mouse and rat models, and helps inhibit myeloma growth.

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

Suvecaltamide Chemical Structure

CAS No. : 953778-58-0

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 75	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 75	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 700	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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View All Calcium Channel Isoform Specific Products:

View All Isoforms

N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

T-type calcium channel

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	1.2 nM Compound: 1; MK-8998	Inhibition of CaV 3.1 channel (unknown origin) expressed in HEK293 cells by FLEPR Ca2+ flux assay Inhibition of CaV 3.1 channel (unknown origin) expressed in HEK293 cells by FLEPR Ca2+ flux assay	[PMID: 27933950]
HEK293	IC₅₀	1.2 nM Compound: 1	Inhibition of T-type calcium channel Cav3.1 (unknown origin) expressed in HEK293 cells assessed as calcium influx by Fluo-4-AM dye-based FLIPR assay Inhibition of T-type calcium channel Cav3.1 (unknown origin) expressed in HEK293 cells assessed as calcium influx by Fluo-4-AM dye-based FLIPR assay	[PMID: 27579577]
HEK293	IC₅₀	1.5 nM Compound: 1; MK-8998	Inhibition of CaV 3.3 channel (unknown origin) expressed in HEK293 cells by FLEPR Ca2+ flux assay Inhibition of CaV 3.3 channel (unknown origin) expressed in HEK293 cells by FLEPR Ca2+ flux assay	[PMID: 27933950]
HEK293	IC₅₀	1.5 nM Compound: 1	Inhibition of T-type calcium channel Cav3.3 (unknown origin) expressed in HEK293 cells assessed as calcium influx by Fluo-4-AM dye-based FLIPR assay Inhibition of T-type calcium channel Cav3.3 (unknown origin) expressed in HEK293 cells assessed as calcium influx by Fluo-4-AM dye-based FLIPR assay	[PMID: 27579577]
HEK293	IC₅₀	8.2 nM Compound: 1; MK-8998	Inhibition of CaV 3.2 channel (unknown origin) expressed in HEK293 cells by FLEPR Ca2+ flux assay Inhibition of CaV 3.2 channel (unknown origin) expressed in HEK293 cells by FLEPR Ca2+ flux assay	[PMID: 27933950]
HEK293	IC₅₀	8.2 nM Compound: 1	Inhibition of recombinant T-type calcium channel Cav3.2 (unknown origin) expressed in HEK293 cells assessed as inhibition of CaCl2-induced calcium influx preincubated for 3 mins prior CaCl2 addition by Fluo-4-AM dye-based FLIPR assay Inhibition of recombinant T-type calcium channel Cav3.2 (unknown origin) expressed in HEK293 cells assessed as inhibition of CaCl2-induced calcium influx preincubated for 3 mins prior CaCl2 addition by Fluo-4-AM dye-based FLIPR assay	[PMID: 27579577]

In Vitro

Suvecaltamide (10-1000 nM, 72 h) does not affect the inhibitory effect of Bortezomib (BTZ, HY-10227) on MM.1S, RPMI 8226, and U266B1 cells.

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

Cell Cytotoxicity Assay^[1]

Cell Line:	Bone marrow cancer cell lines MM.1S, RPMI 8226, U266B1 (cultured for 72 hours with 0.05-250nM BTZ)
Concentration:	10, 30, 100, 300, 1000 nM
Incubation Time:	72 h
Result:	Did not affect the cytotoxicity of BTZ on cells, and using it alone did not impact cell survival.

In Vivo

Suvecaltamide (3-30 mg/kg, once daily for 28 days, orally) reverses the peripheral nerve toxicity (CIPN) induced by Bortezomib (BTZ, HY-10227) in a rat model^[1].
Suvecaltamide (30 mg/kg, once daily for 28 days, orally) reduces tumor volume in a xenograft mouse model of human multiple myeloma without affecting the anti-cancer activity of BTZ^[1].

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

Animal Model:	BTZ-Induced CIPN Rat Model^[1]
Dosage:	3, 10, 30 mg/kg; once daily for 28 days
Administration:	orally
Result:	Increased raised the nerve conduction velocity (NCV) levels of the tail nerve and sciatic nerve by dose-dependent. Reduced the β-tubulin polymerization caused by BTZ and increased the number of cutaneous unmyelinated fiber in the hindpaw (IENF) at 30 mg/kg, without affecting proteasome activity.

Animal Model:	a START cell-based xenograft athymic nude mouse tumor model of human myeloma^[1]
Dosage:	30 mg/kg, once daily for 28 days
Administration:	orally
Result:	Reduced the size of the tumor without affecting the anti-cancer activity of BTZ or the weight loss effects.

Clinical Trial

Molecular Weight

380.40

Formula

C₂₀H₂₃F₃N₂O₂

CAS No.

953778-58-0

Appearance

Solid

Color

White to off-white

SMILES

O=C(N[C@@H](C1=NC=C(OCC(F)(F)F)C=C1)C)CC2=CC=C(C(C)C)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (262.88 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	2.6288 mL	13.1441 mL	26.2881 mL
5 mM	0.5258 mL	2.6288 mL	5.2576 mL
10 mM	0.2629 mL	1.3144 mL	2.6288 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.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 (6.57 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 (6.57 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)

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.

Purity & Documentation

Purity: 99.96%

Select Batch:

Data Sheet (271 KB) SDS (393 KB)

COA (244 KB) LCMS (83 KB)

Handling Instructions (2659 KB)

References

[1]. Cristina Meregalli, et al. Reversal of Bortezomib-Induced Neurotoxicity by Suvecaltamide, a Selective T-Type Ca-Channel Modulator, in Preclinical Models. Cancers (Basel). 2021 Oct 7;13(19):5013. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6288 mL	13.1441 mL	26.2881 mL	65.7203 mL
	5 mM	0.5258 mL	2.6288 mL	5.2576 mL	13.1441 mL
	10 mM	0.2629 mL	1.3144 mL	2.6288 mL	6.5720 mL
	15 mM	0.1753 mL	0.8763 mL	1.7525 mL	4.3814 mL
	20 mM	0.1314 mL	0.6572 mL	1.3144 mL	3.2860 mL
	25 mM	0.1052 mL	0.5258 mL	1.0515 mL	2.6288 mL
	30 mM	0.0876 mL	0.4381 mL	0.8763 mL	2.1907 mL
	40 mM	0.0657 mL	0.3286 mL	0.6572 mL	1.6430 mL
	50 mM	0.0526 mL	0.2629 mL	0.5258 mL	1.3144 mL
	60 mM	0.0438 mL	0.2191 mL	0.4381 mL	1.0953 mL
	80 mM	0.0329 mL	0.1643 mL	0.3286 mL	0.8215 mL
	100 mM	0.0263 mL	0.1314 mL	0.2629 mL	0.6572 mL

Suvecaltamide Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
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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Suvecaltamide (Synonyms: MK-8998; CX-8998; JZP385)

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Complete Stock Solution Preparation Table

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