Referencia número: HY-101096

Suvecaltamide

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

Revisión del cliente

Based on 1 Customer Validation

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.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 99.96%
No. CAS: 953778-58-0
Fòrmula: C₂₀H₂₃F₃N₂O₂
Peso molecular:380.40

Almacenamiento:

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

Suvecaltamide Chemical Structure

No. CAS: 953778-58-0

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

T-type calcium channel

Ver todos los productos específicos de isoformas Calcium Channel :

Cellular Effect

Cell Line	Type	Value	Description	References
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	1.2 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	1.5 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	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	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]
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]

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.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 953778-58-0
Appearance Solid
Peso molecular 380.40
Fòrmula C₂₀H₂₃F₃N₂O₂
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
Synonyms

MK-8998; CX-8998; JZP385
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Solvente y solubilidad

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (271 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	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

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Suvecaltamide

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Neuroprotective Compound Library

Anti-Blood Cancer Compound Library

Calcium Channel Blocker Library

Heterocyclic Compound Library

Pain-Related Compound Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Ver todos los productos específicos de isoformas Calcium Channel

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Suvecaltamide

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Neuroprotective Compound Library

Anti-Blood Cancer Compound Library

Calcium Channel Blocker Library

Heterocyclic Compound Library

Pain-Related Compound Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Ver todos los productos específicos de isoformas Calcium Channel

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Suvecaltamide Related Classifications

HY-101096 Related Classifications