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LHVS (K110717) is a novel, potent, non-selective and irreversible cysteine protease cathepsin S (CatS) inhibitor. LHVS effectively blocks T. gondii microneme protein secretion (IC50=10 μM), gliding motility, and cell invasion.
| ln Vitro |
When compared to untreated osteoclasts, LHVS (5 μM, 2 hours) caused a 50% decrease in actin ring formation in wild-type osteoclasts [1]. LHVS inhibits cathepsins K, L, S, and B at 5 μM and acts on osteoclasts in a dose-dependent manner [1]. In HOM2 cells, LHVS (1–5 nM) selectively inhibits cathepsin S, maintaining the functional activity of other cysteine proteases [3]. By stopping micronemes from releasing at least two essential invasion proteins, MIC2 and M2AP, LHVS hinders tachyzoite attachment [2]. LHVS (50 μM) specifically reduces the secretion of microsomal proteins [2].
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| ln Vivo |
In neuropathic rats, LHVS (3–30 mg/kg, subcutaneous injection, once) exhibits anti-hyperalgesic effects [4]. Neuropathic rats show analgesic effects from daily spinal administration of 30 nmol per rat of LHVS [5]. In 14-day-old neuropathic rats, LHVS (1-50 nmol per rat, intrathecally, daily) reverses established neuropathic mechanical hyperalgesia [5].
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| Animal Protocol |
Animal/Disease Models: Male Wistar rat (180-220 g) [4]
Doses: 3-30 mg/kg Route of Administration: subcutaneous injection, once Experimental Results:Produces dose-dependent reversal of mechanical hyperalgesia, long-lasting in neuropathic rats up to 3 hrs (hrs (hours)). In contrast, a single systemic administration of LHVS did not reverse mechanical allodynia in neuropathic rats. Animal/Disease Models: Male Wistar rats received partial ligation of the left sciatic nerve (PNL) [5] Doses: 30 nmol per rat Route of Administration: spinal cord, daily Experimental Results: continuous administration from day 0 to day 1 failed to prevent the occurrence of allodynia on day 7 after PNL, but Dramatically reversed allodynia on day 7 after PNL. Furthermore, LHVS from days 7 to 14 after PNL Dramatically reversed established mechanical allodynia from day 8 onwards. Animal/Disease Models: Male Wistar rats underwent partial ligation of the left sciatic nerve (PNL) [5] Doses: 1. 10 or 50 nmol per rat Route of Administration: Intrathecal injection, daily Experimental Results: Reduction of established mechani |
| References |
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| Molecular Formula |
C28H37N3O5S
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|---|---|
| Molecular Weight |
527.675486326218
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| Exact Mass |
527.245
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| CAS # |
170111-28-1
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| PubChem CID |
5287864
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| Appearance |
White to off-white solid powder
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| LogP |
3.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
37
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| Complexity |
836
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| Defined Atom Stereocenter Count |
2
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| SMILES |
[C@@H](CC(C)C)(NC(N1CCOCC1)=O)C(=O)N[C@@H](CCC1C=CC=CC=1)/C=C/S(C1C=CC=CC=1)(=O)=O
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| InChi Key |
YUMYYTORLYHUFW-ZUDLOMHPSA-N
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| InChi Code |
InChI=1S/C28H37N3O5S/c1-22(2)21-26(30-28(33)31-16-18-36-19-17-31)27(32)29-24(14-13-23-9-5-3-6-10-23)15-20-37(34,35)25-11-7-4-8-12-25/h3-12,15,20,22,24,26H,13-14,16-19,21H2,1-2H3,(H,29,32)(H,30,33)/b20-15+/t24-,26-/m1/s1
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| Chemical Name |
N-[(2R)-1-[[(E,3R)-1-(Benzenesulfonyl)-5-phenylpent-1-en-3-yl]amino]-4-methyl-1-oxopentan-2-yl]morpholine-4-carboxamide
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| Synonyms |
K-110717 K 110717 K110717
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~189.51 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.74 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (4.74 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.74 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8951 mL | 9.4754 mL | 18.9509 mL | |
| 5 mM | 0.3790 mL | 1.8951 mL | 3.7902 mL | |
| 10 mM | 0.1895 mL | 0.9475 mL | 1.8951 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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