| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
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| ln Vitro |
PTP1B(1-405) is inactive for extended periods of time, but DPM-1001 reversibly inhibits PTP1B in its short form. DPM-1001 has an IC50 value of 600 nM for PTP1B(1-405) and targets PTP1B(1-405) without preincubation. But following a half-hour preincubation, the potency rose to 100 nM. On the other hand, the IC50 value of PTP1B(1-321)[1] does not appear to vary with time.
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|---|---|
| ln Vivo |
By enhancing insulin and leptin signaling, DPM-1001 (orally or intraperitoneally; 5 mg/kg; once daily; 50 days) prevents diet-induced obesity in rats. Within five days of receiving DPM-1001 therapy and a high-fat diet, mice started to lose weight. Approximately three weeks pass during which time weight loss stops [1].
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| Animal Protocol |
Animal/Disease Models: 18weeks old, high-fat diet (HFD)-fed obese male mice (C57bl6/J) [1]
Doses: 5 mg/kg Route of Administration: oral or intraperitoneal (ip) injection; 5 mg/kg; one time/day; 50 day Experimental Results: 5% weight loss. Improves glucose tolerance and insulin sensitivity in the body. |
| References |
| Molecular Formula |
C35H57N3O3
|
|---|---|
| Molecular Weight |
567.845390081406
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| Exact Mass |
567.44
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| CAS # |
1471172-27-6
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| Related CAS # |
DPM-1001 trihydrochloride
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| PubChem CID |
139291002
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| Appearance |
Light yellow to brown solid powder
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| LogP |
6.2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
41
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| Complexity |
855
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| Defined Atom Stereocenter Count |
10
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| SMILES |
O[C@@H]1C[C@H]2C[C@@H](CC[C@]2(C)[C@H]2CC[C@]3(C)[C@@H]([C@H](C)CCC(=O)OC)CC[C@H]3[C@@H]21)NCCCCNCC1C=CC=CN=1
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| InChi Key |
RVANDQULNPITCN-MCVYBXALSA-N
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| InChi Code |
InChI=1S/C35H57N3O3/c1-24(10-13-32(40)41-4)28-11-12-29-33-30(15-17-35(28,29)3)34(2)16-14-26(21-25(34)22-31(33)39)37-20-8-7-18-36-23-27-9-5-6-19-38-27/h5-6,9,19,24-26,28-31,33,36-37,39H,7-8,10-18,20-23H2,1-4H3/t24-,25-,26-,28-,29+,30+,31-,33+,34+,35-/m1/s1
|
| Chemical Name |
methyl (4R)-4-[(3R,5R,7R,8R,9S,10S,13R,14S,17R)-7-hydroxy-10,13-dimethyl-3-[4-(pyridin-2-ylmethylamino)butylamino]-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoate
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| Synonyms |
DPM 1001; DPM1001; DPM-1001
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| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~176.10 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (8.81 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 50.0 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: ≥ 5 mg/mL (8.81 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 50.0 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: ≥ 5 mg/mL (8.81 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 | 1.7610 mL | 8.8051 mL | 17.6103 mL | |
| 5 mM | 0.3522 mL | 1.7610 mL | 3.5221 mL | |
| 10 mM | 0.1761 mL | 0.8805 mL | 1.7610 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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