MDL 28170 | CAS#88191-84-8 | calpain and cathepsin B inhibitor

MedKoo Cat#: 462300 | Name: MDL 28170

Description:

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

MDL 28170 is a potent, selective calpain and cathepsin B inhibitor.

Chemical Structure

MDL 28170

CAS#88191-84-8

Theoretical Analysis

MedKoo Cat#: 462300

Name: MDL 28170

CAS#: 88191-84-8

Chemical Formula: C22H26N2O4

Exact Mass: 382.1893

Molecular Weight: 382.46

Elemental Analysis: C, 69.09; H, 6.85; N, 7.32; O, 16.73

Price and Availability

Size	Price	Availability
100mg	USD 950.00	2 Weeks
200mg	USD 1,450.00	2 Weeks
500mg	USD 2,650.00	2 Weeks
1g	USD 3,650.00	2 Weeks
2g	USD 6,450.00	2 Weeks

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Synonym

MDL 28170; MDL28170; MDL-28170; Calpain Inhibitor III

IUPAC/Chemical Name

benzyl ((2S)-3-methyl-1-oxo-1-((1-oxo-3-phenylpropan-2-yl)amino)butan-2-yl)carbamate

InChi Key

NGBKFLTYGSREKK-ANYOKISRSA-N

InChi Code

InChI=1S/C22H26N2O4/c1-16(2)20(24-22(27)28-15-18-11-7-4-8-12-18)21(26)23-19(14-25)13-17-9-5-3-6-10-17/h3-12,14,16,19-20H,13,15H2,1-2H3,(H,23,26)(H,24,27)/t19?,20-/m0/s1

SMILES Code

[H]C(C(CC1=CC=CC=C1)NC([C@H](C(C)C)NC(OCC2=CC=CC=C2)=O)=O)=O

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

>3 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:

MDL-28170 (Calpain Inhibitor III) is a potent, selective and membrane-permeable cysteine protease inhibitor of calpain that rapidly penetrates the blood-brain barrier following systemic administration. MDL-28170 also block γ-secretase.

In vitro activity:

These results showed that the calpain inhibitor MDL28170 at 15 and 30μM significantly reduced the interaction process of promastigotes with macrophages by 16% and 41%, respectively. The inhibitor was also able to drastically reduce the number of infected macrophages in a time- and dose-dependent manner: after only 24h, MDL28170 was able to significantly diminish the infection rate, presenting an IC50 value of 18.2μM for amastigotes. Reference: Parasitol Int. 2017 Oct;66(5):579-583. https://pubmed.ncbi.nlm.nih.gov/28663009/

In vivo activity:

Diabetic rats demonstrated the mechanical allodynia and thermal hyperalgesia with reduced nerve perfusion and conduction velocity as compared to control. MDL 28170 treatments significantly recovered these functional and nociceptive deficits. MDL 28170 treatments in diabetic rats significantly blocked the altered channel kinetics with hyperpolarizing shift in voltage-dependence of steady-state activation and inactivation curves. Reference: Neuropharmacology. 2015 Oct;97:113-21. https://pubmed.ncbi.nlm.nih.gov/26087461/

	Solvent	mg/mL	mM
Solubility
	DMF	14.0	36.61
	DMF:PBS (pH 7) (1:10)	0.1	0.24
	DMSO	39.5	103.28
	Ethanol	6.7	17.39

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 382.46 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. Marinho FA, Sangenito LS, Oliveira SSC, De Arruda LB, D'Ávila-Levy CM, Santos ALS, Branquinha MH. The potent cell permeable calpain inhibitor MDL28170 affects the interaction of Leishmania amazonensis with macrophages and shows anti-amastigote activity. Parasitol Int. 2017 Oct;66(5):579-583. doi: 10.1016/j.parint.2017.06.010. Epub 2017 Jun 27. PMID: 28663009. 2. Ennes-Vidal V, Menna-Barreto RF, Santos AL, Branquinha MH, d'Avila-Levy CM. Effects of the calpain inhibitor MDL28170 on the clinically relevant forms of Trypanosoma cruzi in vitro. J Antimicrob Chemother. 2010 Jul;65(7):1395-8. doi: 10.1093/jac/dkq154. Epub 2010 May 10. PMID: 20457672. 3. Kharatmal SB, Singh JN, Sharma SS. Calpain inhibitor, MDL 28170 confer electrophysiological, nociceptive and biochemical improvement in diabetic neuropathy. Neuropharmacology. 2015 Oct;97:113-21. doi: 10.1016/j.neuropharm.2015.05.040. Epub 2015 Jun 15. PMID: 26087461. 4. Tona Y, Hamaguchi K, Ishikawa M, Miyoshi T, Yamamoto N, Yamahara K, Ito J, Nakagawa T. Therapeutic potential of a gamma-secretase inhibitor for hearing restoration in a guinea pig model with noise-induced hearing loss. BMC Neurosci. 2014 May 22;15:66. doi: 10.1186/1471-2202-15-66. PMID: 24884926; PMCID: PMC4051152.

In vitro protocol:

In vivo protocol:

1. Kharatmal SB, Singh JN, Sharma SS. Calpain inhibitor, MDL 28170 confer electrophysiological, nociceptive and biochemical improvement in diabetic neuropathy. Neuropharmacology. 2015 Oct;97:113-21. doi: 10.1016/j.neuropharm.2015.05.040. Epub 2015 Jun 15. PMID: 26087461. 2. Tona Y, Hamaguchi K, Ishikawa M, Miyoshi T, Yamamoto N, Yamahara K, Ito J, Nakagawa T. Therapeutic potential of a gamma-secretase inhibitor for hearing restoration in a guinea pig model with noise-induced hearing loss. BMC Neurosci. 2014 May 22;15:66. doi: 10.1186/1471-2202-15-66. PMID: 24884926; PMCID: PMC4051152.

1: Chen ZF, Schottler F, Lee KS. Neuronal recovery after moderate hypoxia is improved by the calpain inhibitor MDL28170. Brain Res. 1997;769(1):188-192. doi:10.1016/s0006-8993(97)00848-2 2: Li PA, Howlett W, He QP, Miyashita H, Siddiqui M, Shuaib A. Postischemic treatment with calpain inhibitor MDL 28170 ameliorates brain damage in a gerbil model of global ischemia. Neurosci Lett. 1998;247(1):17-20. doi:10.1016/s0304-3940(98)00266-3 3: Mehdi S. Cell-penetrating inhibitors of calpain. Trends Biochem Sci. 1991;16(4):150-153. doi:10.1016/0968-0004(91)90058-4 4: Ai J, Liu E, Wang J, Chen Y, Yu J, Baker AJ. Calpain inhibitor MDL-28170 reduces the functional and structural deterioration of corpus callosum following fluid percussion injury. J Neurotrauma. 2007;24(6):960-978. doi:10.1089/neu.2006.0224