SID 26681509

Product Name: SID 26681509
CAS No.: 958772-66-2
Chemical Name: SID 26681509
Synonyms: ML023;SID 26681509;SID26681509; SID-26681509;N-[(1,1-Dimethylethoxy)carbonyl]-L-tryptophan-2-[[[2-[(2-ethylphenyl)amino]-2-oxoethyl]thio]carbonyl]hydrazide;L-Tryptophan, N-[(1,1-dimethylethoxy)carbonyl]-, 2-[[[2-[(2-ethylphenyl)amino]-2-oxoethyl]thio]carbonyl]hydrazide;S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] [2-[(2S)-3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]hydrazinyl]methanethioate;slow-binding,falciparu,Inhibitor,SID-26681509,propagation,Parasite,Leishmania,major,reversible,Cathepsin,inhibit,SID26681509,Plasmodium,malaria,SID 26681509,Thiocarbazate
CBNumber: CB82535696
Molecular Formula: C27H33N5O5S
Formula Weight: 539.65
MOL File: 958772-66-2.mol

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SID 26681509 Property

Melting point:: 131 °C
Density: 1.298±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: <26.98mg/ml in DMSO; <5.4mg/ml in ethanol
form: solid
pka: 8.75±0.43(Predicted)
color: White

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Tocris

Product number: 3625
Product name: SID26681509
Purity: ≥97%(HPLC)
Packaging: 10
Price: $236
Updated: 2021/12/16

Tocris

Product number: 3625
Product name: SID26681509
Purity: ≥97%(HPLC)
Packaging: 50
Price: $992
Updated: 2021/12/16

TRC

Product number: S422805
Product name: SID26681509
Packaging: 10mg
Price: $215
Updated: 2021/12/16

TRC

Product number: S422805
Product name: SID26681509
Packaging: 50mg
Price: $905
Updated: 2021/12/16

ChemScene

Product number: CS-0027706
Product name: SID26681509
Purity: ≥98.0%
Packaging: 10mg
Price: $980
Updated: 2021/12/16

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SID 26681509 Chemical Properties,Usage,Production

Uses

SID 26681509 is a small molecule cathespin L inhibitor.

Definition

ChEBI: SID 26681509 is a carbohydrazide that is L-tryptophan in which the amino and carboxy groups are substituted by tert-butoxycarbonyl and 2-({[2-(2-ethylanilino)-2-oxoethyl]sulfanyl}carbonyl)hydrazinyl groups, respectively. It is a potent and reversible inhibitor of human cathepsin L (IC50 = 56 nM). It has a role as a cathepsin L (EC 3.4.22.15) inhibitor and an antiplasmodial drug. It is a secondary carboxamide, a L-tryptophan derivative, a tert-butyl ester, a thioester and a carbohydrazide.

Biological Activity

sid 26681509 is a potent and reversible human cathepsin l inhibitor.the cathepsins have been found to comprise a family of lysosomal protease enzymes whose primary functions, such as protein degradation, play a keyl role in normal cellular homeostasis. overexpression of cathepsin l and/or abnormal activity has been implicated in a number of disease states.

in vitro

sid 26681509 was found to inhibit human cathepsin l with an ic50 of 56 nm. after preincubation with enzyme for 1, 2, and 4 h before substrate addition, sid 26681509 showed increasing potency, with ic50 values falling to 7.5, 4.2, and 1.0 nm, respectively, indicating a slow onset of inhibition. sid 26681509 was also observed to be nontoxic to human aortic endothelial cells up to 100 μm. sid 26681509 was active in an in vitro propagation assay against p. falciparum with an ic50 of 15.4 μm. additionally, the thiocarbazate inhibitor was toxic toward l. major promastigotes with an ic50 of 12.5 μm [1].

in vivo

sid 26681509 showed a lack of toxicity to zebrafish in a live organism assay at 100 μm [1].

IC 50

56 nm

storage

Store at -20°C

References

[1] shah pp,myers mc,beavers mp,purvis je,jing h,grieser hj,sharlow er,napper ad,huryn dm,cooperman bs,smith ab 3rd,diamond sl. kinetic characterization and molecular docking of a novel, potent, and selective slow-binding inhibitor of human cathepsin l. mol pharmacol.2008 jul;74(1):34-41.

SID 26681509 Preparation Products And Raw materials

Raw materials

Preparation Products

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SID 26681509 Suppliers

China 36 United Kingdom 1 United States 8 Global 45

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958772-66-2, SID 26681509Related Search:

S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] [2-[(2S)-3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]hydrazinyl]methanethioate

N-[(1,1-Dimethylethoxy)carbonyl]-L-tryptophan-2-[[[2-[(2-ethylphenyl)amino]-2-oxoethyl]thio]carbonyl]hydrazide

SID 26681509

SID26681509; SID-26681509

ML023

slow-binding,falciparu,Inhibitor,SID-26681509,propagation,Parasite,Leishmania,major,reversible,Cathepsin,inhibit,SID26681509,Plasmodium,malaria,SID 26681509,Thiocarbazate

L-Tryptophan, N-[(1,1-dimethylethoxy)carbonyl]-, 2-[[[2-[(2-ethylphenyl)amino]-2-oxoethyl]thio]carbonyl]hydrazide

958772-66-2