| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
PDE5 2.28 nM (IC50) PDE6 45.2 nM (IC50) PDE1 566 nM (IC50) PDE4 834 nM (IC50) PDE11 6090 nM (IC50)
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|---|---|
| ln Vivo |
The intracavernous pressure/blood pressure ratio (ICP/BP) was elevated at all time points at the 5.0 mg/kg dose, 75, 90, 105, and 2.5 mg/kg by TPN729MA (1.25, 2.5, 5.0 mg/kg; 1 dose). elevated blood pressure to intracavernous pressure ratio at 120 minutes[1]. In male beagle dogs, TPN729MA (5.0 μg/kg; administered intravenously) dramatically raises both intracavernous pressure and the intracavernous pressure/blood pressure ratio[1].
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| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats with corpora cavernosa complete exposure[1]
Doses: 1.25, 2.5 and 5.0 mg/kg Route of Administration: Intraduodenal (id) injection; 1.25, 2.5 and 5.0 mg/kg, once Experimental Results: Dose-dependently increased the maximum intracavernous pressure (ICP) and ICP/blood pressure (BP). |
| References |
[1]. Wang Z, et al. The selectivity and potency of the new PDE5 inhibitor TPN729MA. J Sex Med. 2013 Nov;10(11):2790-7.
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| Molecular Formula |
C29H40N6O8S
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|---|---|
| Molecular Weight |
632.73
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| CAS # |
1422955-52-9
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| Related CAS # |
TPN729;936951-20-1
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| SMILES |
C1(C2N(C)N=C(CCC)C=2NC(C2C=C(C=CC=2OCCC)S(=O)(N(C)CCN2CCCC2)=O)=N1)=O.OC(=O)/C=C\C(=O)O
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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 and light. |
| 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: 25 mg/mL (39.51 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.95 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 (3.95 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 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 (3.95 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 | 1.5805 mL | 7.9023 mL | 15.8045 mL | |
| 5 mM | 0.3161 mL | 1.5805 mL | 3.1609 mL | |
| 10 mM | 0.1580 mL | 0.7902 mL | 1.5805 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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