Size | Price | |
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500mg | ||
1g | ||
Other Sizes |
ln Vitro |
J-2156 shows over 400-fold subtype selectivity for other somatostatin receptors (h sst1: Ki = 1.2 nM; h sst2: Ki >5000 nM; h sst3: Ki = 1400 nM; h sst5: Ki = 540 nM) in Chinese hamster ovary (CHO) cells and binds to human somatostatin receptor subtype 4 (h sst4: Ki=1.2 nM) with nanomolar affinity [2].
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ln Vivo |
In rats with BCIBP, a single intraperitoneal bolus dosage of J-2156 (1–10 mg/kg) produces both contralateral and ipsilateral anti-allodynic effects [1].
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Animal Protocol |
Animal/Disease Models: Breast Cancer Induced Bone Pain (BCIBP)-Rat[1]
Doses: 1, 3, 10 mg/kg Dosing: IP; 3 hrs (hrs (hours)) Experimental Results: Ipsilateral and contralateral to BCIBP rats Allodynic effects. |
References |
Molecular Formula |
C26H29F3N4O6S
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Molecular Weight |
582.59187579155
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Exact Mass |
468.183
|
CAS # |
848647-56-3
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Related CAS # |
J-2156 TFA;2387505-73-7
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PubChem CID |
11442741
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Appearance |
Typically exists as solid at room temperature
|
LogP |
2.2
|
Hydrogen Bond Donor Count |
4
|
Hydrogen Bond Acceptor Count |
6
|
Rotatable Bond Count |
10
|
Heavy Atom Count |
33
|
Complexity |
763
|
Defined Atom Stereocenter Count |
2
|
SMILES |
CC1=CC=C(C2=CC=CC=C12)S(=O)(=O)N[C@@H](CCN)C(=O)N[C@@H](CC3=CC=CC=C3)C(=O)N
|
InChi Key |
VTNCZBXJSGKDLS-SFTDATJTSA-N
|
InChi Code |
InChI=1S/C24H28N4O4S/c1-16-11-12-22(19-10-6-5-9-18(16)19)33(31,32)28-20(13-14-25)24(30)27-21(23(26)29)15-17-7-3-2-4-8-17/h2-12,20-21,28H,13-15,25H2,1H3,(H2,26,29)(H,27,30)/t20-,21-/m0/s1
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Chemical Name |
(2S)-4-amino-N-[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]-2-[(4-methylnaphthalen-1-yl)sulfonylamino]butanamide
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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 : ~250 mg/mL (~533.54 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.44 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 20.8 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: ≥ 2.08 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 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: ≥ 2.08 mg/mL (4.44 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 | 1.7165 mL | 8.5824 mL | 17.1647 mL | |
5 mM | 0.3433 mL | 1.7165 mL | 3.4329 mL | |
10 mM | 0.1716 mL | 0.8582 mL | 1.7165 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.