| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
The concentration-dependent reduction of U-87, U-138, and A-172 cell viability is observed with KYP-2047 (0-100 μM) [2]. KYP-2047 (0-100 μM) drastically lowers the expression of TGF-β and enhances the production of the pro-apoptotic proteins Bax, p53, and caspase-3, while lowering the expression of Bcl-2 [2].
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| ln Vivo |
In the water maze, KYP-2047 (1 or 5 mg/kg, 30 min before daily testing) dose-dependently enhanced escape performance (i.e., latency to discover the concealed platform and swimming path length) in young but not elderly rats. 1. The hypothalamus's neurotensin concentrations are raised by KYP-2047 (9 or 27 μmol/kg; IP); once, one, or three hours prior to beheading; twice daily for ten days [1]. Tumor mass and neutrophil infiltration are markedly decreased by KYP-2047 (0–5 mg/kg) [2]. The expression of vascular endothelial growth factor (VEGF), CD34, angiopoietin (Ang), and endothelial nitric oxide synthase (eNOS) is dramatically reduced by KYP-2047 (0–5 mg/kg) [2].
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| Cell Assay |
Cell Proliferation Assay
Cell Types: U-87, U-138 and A-172 cells [2] Tested Concentrations: 0.01 μM, 0.1 μM, 0.5 μM, 1 μM, 10 μM, 30 μM, 50 μM and 100 μM Incubation Duration: 24 h Experimental Results: U-87, U-138 and A-172 cell viability diminished in a concentration-dependent manner. Western Blot Analysis Cell Types: U-87 cells [2] Tested Concentrations: 0, 50, 100 μM Incubation Duration: 24 h Experimental Results: The expression of pro-apoptotic proteins Bax, p53 and cleaved-caspase-3 increased, and the expression of Bcl2 Dramatically diminished. Reduces Ang1 and Ang2 expression, and reduces Ki-67 expression. |
| References |
|
| Molecular Formula |
C20H25N3O2
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|---|---|
| Molecular Weight |
339.431404829025
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| Exact Mass |
339.194
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| CAS # |
796874-99-2
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| PubChem CID |
11198569
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| Appearance |
White to off-white solid powder
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| LogP |
2.3
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
25
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| Complexity |
532
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C(N1CCC[C@H]1C#N)([C@@H]1CCCN1C(=O)CCCC1C=CC=CC=1)=O
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| InChi Key |
SPXFAUXQZWJGCJ-ROUUACIJSA-N
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| InChi Code |
InChI=1S/C20H25N3O2/c21-15-17-10-5-13-22(17)20(25)18-11-6-14-23(18)19(24)12-4-9-16-7-2-1-3-8-16/h1-3,7-8,17-18H,4-6,9-14H2/t17-,18-/m0/s1
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| Chemical Name |
(2S)-1-[(2S)-1-(4-phenylbutanoyl)pyrrolidine-2-carbonyl]pyrrolidine-2-carbonitrile
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| Synonyms |
KYP 2047; KYP2047; KYP-2047
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.9461 mL | 14.7306 mL | 29.4612 mL | |
| 5 mM | 0.5892 mL | 2.9461 mL | 5.8922 mL | |
| 10 mM | 0.2946 mL | 1.4731 mL | 2.9461 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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