MK-8998
- Product Name
- MK-8998
- CAS No.
- 953778-58-0
- Chemical Name
- MK-8998
- Synonyms
- MK-8998;CX-8998;CS-2435;Suvecaltamide;MK8998;MK 8998;MK-8998(compound 33);Suvecaltamide (MK-8998);Suvecaltamide, 10 mM in DMSO;(R)-2-(4-isopropylphenyl)-N-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetaMide;inhibit,MK 8998,Calcium Channel,Ca channels,Inhibitor,Suvecaltamide,Ca2+ channels,MK8998
- CBNumber
- CB82516066
- Molecular Formula
- C20H23F3N2O2
- Formula Weight
- 380.4
- MOL File
- 953778-58-0.mol
MK-8998 Property
- Boiling point:
- 510.3±50.0 °C(Predicted)
- Density
- 1.178±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : ≥ 100 mg/mL (262.88 mM);Water : < 0.1 mg/mL (insoluble)
- pka
- 14.27±0.46(Predicted)
- form
- Solid
- color
- White to off-white
- InChI
- InChI=1S/C20H23F3N2O2/c1-13(2)16-6-4-15(5-7-16)10-19(26)25-14(3)18-9-8-17(11-24-18)27-12-20(21,22)23/h4-9,11,13-14H,10,12H2,1-3H3,(H,25,26)/t14-/m1/s1
- InChIKey
- IQIKXZMPPBEWAD-CQSZACIVSA-N
- SMILES
- C1(CC(N[C@@H](C2=NC=C(OCC(F)(F)F)C=C2)C)=O)=CC=C(C(C)C)C=C1
N-Bromosuccinimide Price
- Product number
- CS-6198
- Product name
- MK-8998
- Purity
- 99.94%
- Packaging
- 5mg
- Price
- $90
- Updated
- 2021/12/16
- Product number
- CS-6198
- Product name
- MK-8998
- Purity
- 99.94%
- Packaging
- 10mg
- Price
- $150
- Updated
- 2021/12/16
- Product number
- CS-6198
- Product name
- MK-8998
- Purity
- 99.94%
- Packaging
- 50mg
- Price
- $450
- Updated
- 2021/12/16
- Product number
- API0027468
- Product name
- MK-8998
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $496
- Updated
- 2021/12/16
- Product number
- CS-6198
- Product name
- MK-8998
- Purity
- 99.94%
- Packaging
- 100mg
- Price
- $700
- Updated
- 2021/12/16
MK-8998 Chemical Properties,Usage,Production
Uses
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[1].
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].
| 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. |
IC 50
T-type calcium channel
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. DOI:10.3390/cancers13195013
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