DS16570511 | CAS# | calcium uniporter

MedKoo Cat#: 530956 | Name: DS16570511

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

DS16570511 is a small-molecule inhibitor of the mitochondrial calcium uniporter. DS16570511 dose-dependently inhibited serum-induced mitochondrial Ca2+ influx in HEK293A cells with an IC50 of 7 μM. DS16570511 inhibited Ca2+ uptake of isolated mitochondria from human cells, rat heart and pig heart. Overexpression of hMCU or hMICU1 in HEK293A cells increased mitochondrial Ca2+ influx, and the increases were completely suppressed by the pretreatment with DS16570511. DS16570511 also blocks mitochondrial Ca2+ overload in a Langendorff perfused beating rat heart. Interestingly, DS16570511 increased cardiac contractility without affecting heart rate in the perfused heart.

Chemical Structure

DS16570511

CAS#2446154-84-1

Theoretical Analysis

MedKoo Cat#: 530956

Name: DS16570511

CAS#: 2446154-84-1

Chemical Formula: C30H25Cl2N3O4

Exact Mass: 561.1222

Molecular Weight: 562.45

Elemental Analysis: C, 64.06; H, 4.48; Cl, 12.61; N, 7.47; O, 11.38

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 450.00	2 weeks
10mg	USD 750.00	2 weeks

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Related CAS #

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Synonym

DS16570511; DS-16570511; DS 16570511.

IUPAC/Chemical Name

4-[3-(3-{[3-(2,6-Dichloro-phenyl)-5-methyl-isoxazol-4-ylmethyl]-amino}-benzoyl)-indol-1-yl]-butyric acid

InChi Key

VIWYGRDFHWYDRW-UHFFFAOYSA-N

InChi Code

InChI=1S/C30H25Cl2N3O4/c1-18-22(29(34-39-18)28-24(31)10-5-11-25(28)32)16-33-20-8-4-7-19(15-20)30(38)23-17-35(14-6-13-27(36)37)26-12-3-2-9-21(23)26/h2-5,7-12,15,17,33H,6,13-14,16H2,1H3,(H,36,37)

SMILES Code

O=C(O)CCCN1C=C(C(C2=CC=CC(NCC3=C(C)ON=C3C4=C(Cl)C=CC=C4Cl)=C2)=O)C5=C1C=CC=C5

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

An inhibitor of the mitochondrial calcium uniporter.

In vitro activity:

In addition, DS (DS16570511) inhibited ADP-stimulated mitochondrial respiration and ADP-induced decrease in the mitochondrial membrane potential. It was found that DS inhibited the activity of complex II of the respiratory chain. In the presence of Ca2+, high DS concentrations caused a collapse of the mitochondrial membrane potential. Reference: Biochim Biophys Acta Gen Subj. 2021 May;1865(5):129847. https://pubmed.ncbi.nlm.nih.gov/33453305/

In vivo activity:

These results showed that DS16570511 blocks Ca2+ uptake by the isolated mitochondria in both small and large animals. Because the IC50 of DS16570511 in the human mitochondria (Figure 2b) was smaller than that of pigs and rats (Figures 3b and c), it is possible that DS16570511 more potently inhibits the uniporter of humans than it inhibits the uniporter of pigs or rats. Reference: Cell Death Discov. 2017 Jul 17;3:17045. https://pubmed.ncbi.nlm.nih.gov/28725491/

	Solvent	mg/mL	mM
Solubility
	DMSO	30.0	53.34
	Ethanol	30.0	53.34
	Ethanol:PBS (pH 7.2) (1:1)	0.5	0.89

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 562.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Belosludtsev KN, Sharipov RR, Boyarkin DP, Belosludtseva NV, Dubinin MV, Krasilnikova IA, Bakaeva ZV, Zgodova AE, Pinelis VG, Surin AM. The effect of DS16570511, a new inhibitor of mitochondrial calcium uniporter, on calcium homeostasis, metabolism, and functional state of cultured cortical neurons and isolated brain mitochondria. Biochim Biophys Acta Gen Subj. 2021 May;1865(5):129847. doi: 10.1016/j.bbagen.2021.129847. Epub 2021 Jan 14. PMID: 33453305. 2. Kon N, Murakoshi M, Isobe A, Kagechika K, Miyoshi N, Nagayama T. DS16570511 is a small-molecule inhibitor of the mitochondrial calcium uniporter. Cell Death Discov. 2017 Jul 17;3:17045. doi: 10.1038/cddiscovery.2017.45. PMID: 28725491; PMCID: PMC5511861.

In vitro protocol:

In vivo protocol:

1. Kon N, Murakoshi M, Isobe A, Kagechika K, Miyoshi N, Nagayama T. DS16570511 is a small-molecule inhibitor of the mitochondrial calcium uniporter. Cell Death Discov. 2017 Jul 17;3:17045. doi: 10.1038/cddiscovery.2017.45. PMID: 28725491; PMCID: PMC5511861.

1: Kon N, Murakoshi M, Isobe A, Kagechika K, Miyoshi N, Nagayama T. DS16570511 is a small-molecule inhibitor of the mitochondrial calcium uniporter. Cell Death Discov. 2017 Jul 17;3:17045. doi: 10.1038/cddiscovery.2017.45. eCollection 2017. PubMed PMID: 28725491; PubMed Central PMCID: PMC5511861.