Physicochemical Properties
| Molecular Formula | C69H116N26O15S2 |
| Molecular Weight | 1613.97 |
| Exact Mass | 1612.855 |
| CAS # | 132956-87-7 |
| Related CAS # | A-71915 TFA |
| PubChem CID | 25083020 |
| Appearance | White to off-white solid powder |
| Density | 1.5±0.1 g/cm3 |
| Index of Refraction | 1.698 |
| LogP | -5.73 |
| Hydrogen Bond Donor Count | 22 |
| Hydrogen Bond Acceptor Count | 22 |
| Rotatable Bond Count | 27 |
| Heavy Atom Count | 112 |
| Complexity | 3310 |
| Defined Atom Stereocenter Count | 13 |
| Chemical Name | L-Cysteinamide, L-arginyl-L-cysteinyl-3-cyclohexyl-L-alanylglycylglycyl-L-arginyl-L-isoleucyl-L-alpha-aspartyl-L-arginyl-L-isoleucyl-D-1,2,3,4-tetrahydro-3-isoquinolinecarbonyl-L-arginyl-, cyclic (2-13)-disulfide |
| Synonyms | A-71915 A71915A 71915 |
| 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 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) |
Biological Activity
| ln Vitro | For the circulating GMP assay, A 71915 binds to neuroblastoma NB-OK-1 cells. For circulating GMP synthesis, A 71915 causes a rightward change in the ANP dose-response curve [1]. |
| ln Vivo | A71915 (5 μl; intramuscular injection; male CD-1 mice weighing 25–30 g) had an effect on scratching produced by BNP (1 nmol) and GRP (0.1 nmol) [2]. A 71915 (30 μg/kg/day) reduces blood pressure and inhibits NS-398 [3]. |
| Animal Protocol |
Animal/Disease Models: Rat (male SD (SD (Sprague-Dawley))); body weight 150-180 g [3] Doses: 30 μg/kg/day; infusion for 3 weeks Dosing: via mini-osmotic pump Experimental Results: A 71915 (30 μg/kg/ days) pretreatment attenuated the inhibitory effect of NS-398 on blood pressure. |
| References |
[1]. Discovery of a potent atrial natriuretic peptide antagonist for ANPA receptors in the human neuroblastoma NB-OK-1 cell line. Eur J Pharmacol. 1992;224(2-3):183-188. [2]. Spinal Functions of B-Type Natriuretic Peptide, Gastrin-Releasing Peptide, and Their Cognate Receptors for Regulating Itch in Mice. [3]. Attenuation of renovascular hypertension by cyclooxygenase-2 inhibitor partly through ANP release. Peptides. 2015;69:1-8. |
Solubility Data
| Solubility (In Vitro) | H2O : ≥ 50 mg/mL (~30.98 mM) |
| 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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *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. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.6196 mL | 3.0980 mL | 6.1959 mL | |
| 5 mM | 0.1239 mL | 0.6196 mL | 1.2392 mL | |
| 10 mM | 0.0620 mL | 0.3098 mL | 0.6196 mL |