LHVS
- Product Name
- LHVS
- CAS No.
- 170111-28-1
- Chemical Name
- LHVS
- Synonyms
- LHVS;K-110717 (LHVS);N2-(4-Morpholinylcarbonyl)-N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)-1-penten-3-yl]-L-leucinamide;4-Morpholinecarboxamide, N-[(1S)-3-methyl-1-[[[(1S,2E)-1-(2-phenylethyl)-3-(phenylsulfonyl)-2-propen-1-yl]amino]carbonyl]butyl]-
- CBNumber
- CB25821105
- Molecular Formula
- C28H37N3O5S
- Formula Weight
- 527.68
- MOL File
- 170111-28-1.mol
LHVS Property
- Boiling point:
- 822.7±65.0 °C(Predicted)
- Density
- 1.195±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- pka
- 12.50±0.20(Predicted)
- form
- Solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- CS-0102928
- Product name
- LHVS
- Packaging
- 1mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CS-0102928
- Product name
- LHVS
- Packaging
- 5mg
- Price
- $1050
- Updated
- 2021/12/16
LHVS Chemical Properties,Usage,Production
Uses
LHVS is a potent, non-selective, irreversible, cell-permeable cysteine protease and cathepsin inhibitor. LHVS decreases actin ring formation. LHVS inhibits T. gondii invasion with an IC50 of 10 μM[1][2][3].
Biological Activity
LHVS is an irreversible, potent and selective cathepsin S inhibitor (CatS Ki = 5.9 nM; CatO2/L/B Ki = 0.23/0.72/39 μM, Cruzain Ki = 0.22 μM) th at targets CatS active site thiol for covalent modification via its vinyl sulfone moiety. LHVS is a useful tool for studyting CatS-mediated responses in cultures (typical dosing ranges: 25 nM to 10μM) and in animals in vivo, including CatS-induced itch in mice (30 mg/kg sc.), morphine-induced antinociceptive tolerance in rats (50 nmol/r at itrathetically) and mechanical hyperalgesia in nerve-injured rats (3-30 mg/kg sc.).
in vivo
LHVS (3-30 mg/kg, SC, once) shows anti-hyperalgesic effect in neuropathic rats[4].
LHVS (30 nmol per rat, spinal delivery, daily) is antinociceptive in neuropathic rats[5].
LHVS (1-50 nmol per rat, Intrathecal injection, daily) reverses established neuropathic mechanical hyperalgesia in 14-day neuropathic rats[5].
| Animal Model: | Male Wistar rats (180-220 g)[4] |
| Dosage: | 3-30 mg/kg |
| Administration: | SC, once |
| Result: | Produced a dose-dependent reversal of the mechanical hyperalgesia which lasted up to 3 h in neuropathic rats. In contrast, a single systemic administration of LHVS did not reverse mechanical allodynia in neuropathic rats. |
| Animal Model: | Male Wistar rats received a partial ligation of the left sciatic nerve (PNL)[5] |
| Dosage: | 30 nmol per rat |
| Administration: | Spinal delivery, Daily |
| Result: | Failed to prevent the development of allodynia when continuous delivery from day 0 to day 7 post-PNL, but significantly reversed allodynia on day 7 post-PNL. In addition, the delivery of LHVS from day 7 to day 14 post-PNL significantly reversed established mechanical allodynia from day 8. |
| Animal Model: | Male Wistar rats received a partial ligation of the left sciatic nerve (PNL)[5] |
| Dosage: | 1, 10 or 50 nmol per rat |
| Administration: | Intrathecal injection, Daily |
| Result: | Reduced established mechanical hyperalgesia. This effect was dose-dependent and remained significant until 3 h after administration of the highest dose. |
IC 50
cathepsin S; cathepsin K; cathepsin L; Cathepsin B
References
[1] Wilson SR, et al. Cathepsin K activity-dependent regulation of osteoclast actin ring formation and bone resorption. J Biol Chem. 2009 Jan 23;284(4):2584-92. DOI:10.1074/jbc.M805280200
[2] Teo CF, et al.Cysteine protease inhibitors block Toxoplasma gondii microneme secretion and cell invasion. Antimicrob Agents Chemother. 2007 Feb;51(2):679-88. DOI:10.1128/AAC.01059-06
[3] Riese RJ, et al. Essential role for cathepsin S in MHC class II-associated invariant chain processing and peptide loading. Immunity. 1996 Apr;4(4):357-66. DOI:10.1016/s1074-7613(00)80249-6
[4] Barclay J, et al. Role of the cysteine protease cathepsin S in neuropathic hyperalgesia. Pain. 2007 Aug;130(3):225-234. DOI:10.1016/j.pain.2006.11.017
[5] Clark AK, et al. Inhibition of spinal microglial cathepsin S for the reversal of neuropathic pain. Proc Natl Acad Sci U S A. 2007 Jun 19;104(25):10655-60. DOI:10.1073/pnas.0610811104
LHVS Preparation Products And Raw materials
Raw materials
Preparation Products
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