SJA6017
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MedKoo CAT#: 555125

CAS#: 190274-53-4

Description: SJA6017, also known as Calpain Inhibitor VI, is a calpain inhibitor. Treatment with SJA6017 reduces apoptotic cell death, preserves spinal cord tissue and improves functional outcome. Treating calpain-induced apoptosis with this agent may be a feasible therapeutic strategy for patients with spinal cord injury.


Chemical Structure

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SJA6017
CAS# 190274-53-4

Theoretical Analysis

MedKoo Cat#: 555125
Name: SJA6017
CAS#: 190274-53-4
Chemical Formula: C17H25FN2O4S
Exact Mass: 372.15
Molecular Weight: 372.460
Elemental Analysis: C, 54.82; H, 6.77; F, 5.10; N, 7.52; O, 17.18; S, 8.61

Price and Availability

Size Price Availability Quantity
1mg USD 300 2 weeks
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Synonym: Calpain Inhibitor VI; Calpain Inhibitor 4; Calpain-In-4; SJA6017; SJA-6017; SJA 6017.

IUPAC/Chemical Name: (S)-2-((4-fluorophenyl)sulfonamido)-3-methyl-N-((S)-4-methyl-1-oxopentan-2-yl)butanamide

InChi Key: WSJWUIDLGZAXID-HOCLYGCPSA-N

InChi Code: InChI=1S/C17H25FN2O4S/c1-11(2)9-14(10-21)19-17(22)16(12(3)4)20-25(23,24)15-7-5-13(18)6-8-15/h5-8,10-12,14,16,20H,9H2,1-4H3,(H,19,22)/t14-,16-/m0/s1

SMILES Code: FC1=CC=C(C=C1)S(N[C@@H](C(C)C)C(N[C@H](C=O)CC(C)C)=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: >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:
Biological target: Calpain inhibitor VI is an inhibitor of the calcium-dependent cysteine proteases µ-calpain (calpain-1; IC50 = 7.5 nM) and m-calpain (calpain-2; IC50 = 78 nM). It also inhibits cathepsins B and L (IC50s = 15 and 1.6 nM, respectively). It is selective for these calpains and cathepsins over other cysteine and serine proteases, factor VIIa, factor Xa, trypsin, chymotrypsin, and proteasome.
In vitro activity: SJA6017 demonstrated effective neuroprotection against MPP+-induced damage in spinal motoneurons. In VSC 4.1 cells exposed to the Parkinsonian neurotoxicant MPP+, SJA6017 mitigated the rise in intracellular free Ca2+, reduced the active form of calpain, and prevented increased levels of proteases and their activities. It also diminished elevated levels of reactive oxygen species and partially ameliorated impairment in motor proteins dynein and kinesin caused by MPP+. Reference: Neurotox Res. 2020 Oct;38(3):640-649. https://pubmed.ncbi.nlm.nih.gov/32761446/
In vivo activity: SJA6017 may have potential in spinal cord injury treatment. In a rat spinal cord injury model, SJA6017 reduced apoptotic cell death, preserved spinal cord tissue and improved functional outcome. SJA6017 treated rats had significantly reduced tissue injury and had ameliorated recovery of limb function. Reference: J Clin Neurosci. 2008 Oct;15(10):1130-6. https://pubmed.ncbi.nlm.nih.gov/18656362/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 5.0 13.42

Preparing Stock Solutions

The following data is based on the product molecular weight 372.46 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.

Recalculate based on batch purity %
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. Samantaray S, Knaryan VH, M Del Re A, Woodward JJ, Shields DC, Azuma M, Inoue J, Ray SK, Banik NL. Cell-Permeable Calpain Inhibitor SJA6017 Provides Functional Protection to Spinal Motoneurons Exposed to MPP. Neurotox Res. 2020 Oct;38(3):640-649. doi: 10.1007/s12640-020-00264-3. Epub 2020 Aug 6. PMID: 32761446; PMCID: PMC9453439. 2. Biswas S, Harris F, Singh J, Phoenix DA. The in vitro retardation of porcine cataractogenesis by the calpain inhibitor, SJA6017. Mol Cell Biochem. 2004 Jun;261(1-2):169-73. doi: 10.1023/b:mcbi.0000028752.89886.43. PMID: 15362500. 3. Akdemir O, Uçankale M, Karaoğlan A, Barut S, Sağmanligil A, Bilguvar K, Cirakoğlu B, Sahan E, Colak A. Therapeutic efficacy of SJA6017, a calpain inhibitor, in rat spinal cord injury. J Clin Neurosci. 2008 Oct;15(10):1130-6. doi: 10.1016/j.jocn.2007.08.011. Epub 2008 Jul 24. PMID: 18656362. 4. Tamada Y, Fukiage C, Mizutani K, Yamaguchi M, Nakamura Y, Azuma M, Shearer TR. Calpain inhibitor, SJA6017, reduces the rate of formation of selenite cataract in rats. Curr Eye Res. 2001 Apr;22(4):280-5. doi: 10.1076/ceyr.22.4.280.5505. PMID: 11462167.
In vitro protocol: 1. Samantaray S, Knaryan VH, M Del Re A, Woodward JJ, Shields DC, Azuma M, Inoue J, Ray SK, Banik NL. Cell-Permeable Calpain Inhibitor SJA6017 Provides Functional Protection to Spinal Motoneurons Exposed to MPP. Neurotox Res. 2020 Oct;38(3):640-649. doi: 10.1007/s12640-020-00264-3. Epub 2020 Aug 6. PMID: 32761446; PMCID: PMC9453439. 2. Biswas S, Harris F, Singh J, Phoenix DA. The in vitro retardation of porcine cataractogenesis by the calpain inhibitor, SJA6017. Mol Cell Biochem. 2004 Jun;261(1-2):169-73. doi: 10.1023/b:mcbi.0000028752.89886.43. PMID: 15362500.
In vivo protocol: 1. Akdemir O, Uçankale M, Karaoğlan A, Barut S, Sağmanligil A, Bilguvar K, Cirakoğlu B, Sahan E, Colak A. Therapeutic efficacy of SJA6017, a calpain inhibitor, in rat spinal cord injury. J Clin Neurosci. 2008 Oct;15(10):1130-6. doi: 10.1016/j.jocn.2007.08.011. Epub 2008 Jul 24. PMID: 18656362. 2. Tamada Y, Fukiage C, Mizutani K, Yamaguchi M, Nakamura Y, Azuma M, Shearer TR. Calpain inhibitor, SJA6017, reduces the rate of formation of selenite cataract in rats. Curr Eye Res. 2001 Apr;22(4):280-5. doi: 10.1076/ceyr.22.4.280.5505. PMID: 11462167.

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1: Akdemir O, Uçankale M, Karaoğlan A, Barut S, Sağmanligil A, Bilguvar K, Cirakoğlu B, Sahan E, Colak A. Therapeutic efficacy of SJA6017, a calpain inhibitor, in rat spinal cord injury. J Clin Neurosci. 2008 Oct;15(10):1130-6. doi: 10.1016/j.jocn.2007.08.011. Epub 2008 Jul 24. PubMed PMID: 18656362.

2: Biswas S, Harris F, Singh J, Phoenix DA. The in vitro retardation of porcine cataractogenesis by the calpain inhibitor, SJA6017. Mol Cell Biochem. 2004 Jun;261(1-2):169-73. PubMed PMID: 15362500.

3: Inoue J, Nakamura M, Cui YS, Sakai Y, Sakai O, Hill JR, Wang KK, Yuen PW. Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor. J Med Chem. 2003 Feb 27;46(5):868-71. PubMed PMID: 12593666.

4: Kupina NC, Nath R, Bernath EE, Inoue J, Mitsuyoshi A, Yuen PW, Wang KK, Hall ED. The novel calpain inhibitor SJA6017 improves functional outcome after delayed administration in a mouse model of diffuse brain injury. J Neurotrauma. 2001 Nov;18(11):1229-40. PubMed PMID: 11721741.

5: Tamada Y, Fukiage C, Mizutani K, Yamaguchi M, Nakamura Y, Azuma M, Shearer TR. Calpain inhibitor, SJA6017, reduces the rate of formation of selenite cataract in rats. Curr Eye Res. 2001 Apr;22(4):280-5. PubMed PMID: 11462167.

6: Fukiage C, Azuma M, Nakamura Y, Tamada Y, Nakamura M, Shearer TR. SJA6017, a newly synthesized peptide aldehyde inhibitor of calpain: amelioration of cataract in cultured rat lenses. Biochim Biophys Acta. 1997 Oct 24;1361(3):304-12. PubMed PMID: 9375805.