| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| Other Sizes |
| Targets |
VH 101, acid targets the von-Hippel-Lindau (VHL) protein, which is a substrate recognition component of an E3 ubiquitin ligase complex. By binding to VHL, this molecule can recruit the E3 ligase machinery to a protein of interest when conjugated to a target-binding ligand, leading to the ubiquitination and degradation of that target protein.
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|---|---|
| ln Vitro |
In vitro activity of VH 101, acid is not characterized as a pharmacological agent, as it is a synthetic building block. Its primary in vitro application is in the synthesis of PROTAC molecules. The compound is used in chemical conjugation reactions to attach to target protein-binding ligands. The resulting PROTACs are then tested for their ability to induce degradation.
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| ln Vivo |
In vivo activity is not applicable to VH 101, acid, as it is a synthetic building block. The PROTAC molecules synthesized from it may be evaluated in vivo, but VH 101, acid itself is not administered as a drug.
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| Enzyme Assay |
In vitro enzyme or receptor binding assay protocols are not directly applicable to VH 101, acid. However, the VHL-binding activity of the final PROTAC molecules can be assessed using surface plasmon resonance (SPR) or other biophysical methods. The compound is primarily characterized by analytical techniques such as NMR and mass spectrometry.
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| Cell Assay |
In vitro cell-based assay protocols are not directly applicable to VH 101, acid. The PROTAC molecules synthesized from it are evaluated in cell-based assays for their ability to degrade target proteins, typically by Western blot.
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| Animal Protocol |
In vivo animal experimental protocols are not applicable to VH 101, acid. PROTAC molecules synthesized from it may be evaluated in vivo, but VH 101, acid itself is not used in animal studies.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties are not applicable to VH 101, acid as a directly administered compound, as it is a synthetic building block. It is stored at 4°C under nitrogen.
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| References | |
| Additional Infomation |
VH 101, acid is a research-grade compound used as a building block for PROTAC synthesis. It has not entered clinical trials and is not approved for any therapeutic indication. Its mechanism of action is indirect: it enables the recruitment of the VHL E3 ubiquitin ligase to target proteins when incorporated into a PROTAC molecule. The compound is available exclusively for research purposes.
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| Molecular Formula |
C28H35FN4O6S
|
|---|---|
| Molecular Weight |
574.66
|
| Exact Mass |
574.226
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| CAS # |
2408341-97-7
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| PubChem CID |
156701284
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| Appearance |
White to off-white solid powder
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| LogP |
2.6
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| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
40
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| Complexity |
980
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| Defined Atom Stereocenter Count |
4
|
| SMILES |
CC1=C(SC=N1)C2=CC=C(C=C2)[C@H](CC(=O)O)NC(=O)[C@@H]3C[C@H](CN3C(=O)[C@H](C(C)(C)C)NC(=O)C4(CC4)F)O
|
| InChi Key |
IWPNYGPPFCLKCL-QTDGGUCWSA-N
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| InChi Code |
InChI=1S/C28H35FN4O6S/c1-15-22(40-14-30-15)17-7-5-16(6-8-17)19(12-21(35)36)31-24(37)20-11-18(34)13-33(20)25(38)23(27(2,3)4)32-26(39)28(29)9-10-28/h5-8,14,18-20,23,34H,9-13H2,1-4H3,(H,31,37)(H,32,39)(H,35,36)/t18-,19+,20+,23-/m1/s1
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| Chemical Name |
(3S)-3-[[(2S,4R)-1-[(2S)-2-[(1-fluorocyclopropanecarbonyl)amino]-3,3-dimethylbutanoyl]-4-hydroxypyrrolidine-2-carbonyl]amino]-3-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]propanoic acid
|
| 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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
Typically soluble in DMSO (e.g. 10 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7402 mL | 8.7008 mL | 17.4016 mL | |
| 5 mM | 0.3480 mL | 1.7402 mL | 3.4803 mL | |
| 10 mM | 0.1740 mL | 0.8701 mL | 1.7402 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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