| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
| Targets |
Selepressin selectively targets the vasopressin V1A receptor. As a full agonist, it activates the V1A receptor, leading to vasoconstriction and an increase in blood pressure. Its selectivity for the V1A receptor over other vasopressin receptor subtypes contributes to its specific pharmacological profile.
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| ln Vitro |
HLMVEC barrier failure brought on by thrombin or VEGF is ameliorated by SELPRESTIN (100 nM, 48 or 72 hours) [3]. In HLMVEC, selepressin (1-1000 nM, 72 hours) inhibits the loss of cortical actin and VE-cadherin caused by LPS [3]. In HLMVEC, selepressin (100 nM, 48 h) stimulates the production of p53 that protects the barrier [3].
In vitro, Selepressin acts as a selective agonist at the vasopressin V1A receptor. Its binding affinity and functional activity at the V1A receptor have been characterized, demonstrating its potency and selectivity. Detailed in vitro potency data (e.g., EC50) are not provided in the available sources. |
| ln Vivo |
Inhibin (1 μg/kg/min) injected into the left jugular vein for 12 minutes caused a 38.5% increase in mean arterial pressure (MAP) in an LPS-induced fluid-resuscitated rabbit endotoxemia model [2]. In sheep suffering from severe sepsis, vascular leakage is prevented by administering selective vasopressin (7 pmol/kg/min, 10 μL/min) intravenously [4].
In vivo, Selepressin is a potent vasopressor, increasing blood pressure through V1A receptor-mediated vasoconstriction. It is being studied for its potential to treat vasodilatory hypotension in septic shock, a condition where vasopressin levels are often insufficient. Its short half-life allows for rapid titration of its effects. |
| Enzyme Assay |
In vitro receptor binding assays for Selepressin involve measuring its affinity for the vasopressin V1A receptor. Radioligand binding studies using membranes from cells expressing the receptor and a labeled V1A ligand are performed to determine the compound's binding affinity (Ki). Functional activity is assessed by measuring receptor-mediated signaling, such as calcium mobilization or cAMP modulation, in cells expressing the V1A receptor.
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: HLMVEC Tested Concentrations: 1, 10, 100, 1000 nM Incubation Duration: 24 hrs (hours), 48 hrs (hours) Experimental Results: Induced p53 expression levels, but only after 48 hrs (hours) of 100 nM treatment. In vitro cellular assays for Selepressin are performed using cell lines expressing the vasopressin V1A receptor. Cells are treated with the compound, and downstream signaling pathways, such as calcium influx or MAPK activation, are measured to quantify the compound's agonistic activity and potency. These assays help confirm its full agonist profile at the V1A receptor. |
| Animal Protocol |
Animal/Disease Models: LPS-induced fluid resuscitation rabbit endotoxemia model [2].
Doses: 1 μg/kg/min Route of Administration: Left jugular vein infusion over 12 minutes Experimental Results: Mesenteric blood flow (MBF) diminished and mesenteric vascular resistance increased in non-endotoxemic and endotoxemic rabbits. In vivo animal studies for Selepressin are conducted in animal models of septic shock or vasodilatory hypotension. The compound is administered intravenously, and its effects on blood pressure, heart rate, and systemic vascular resistance are measured. Its short half-life and efficacy in restoring hemodynamic stability are evaluated in these models. |
| ADME/Pharmacokinetics |
Selepressin is a peptide with a short half-life, which is a key feature for its potential use in the intensive care setting where rapid titration of vasopressor effects is required. It is administered intravenously. Its PK profile would include rapid onset and offset of action, allowing for precise hemodynamic control.
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| Toxicity/Toxicokinetics |
Toxicological data for Selepressin are not detailed in publicly available sources. As a peptide, its toxicity profile would be expected to be related to its pharmacological effects (vasoconstriction) and potential off-target effects. Standard preclinical safety assessments would have been conducted as part of its development.
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| References |
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| Additional Infomation |
Selepressin is currently in research trials for the treatment of septic shock.
Drug Indications Treatment of septic shock Selepressin is also known as FE 202158. It is a selective vasopressin V1A receptor agonist. It is an analog of vasopressin. It is being developed by Ferring Pharmaceuticals for the treatment of vasodilatory hypotension in septic shock. It has not yet received regulatory approval. |
| Molecular Formula |
C46H73N13O11S2
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|---|---|
| Molecular Weight |
1048.29
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| Exact Mass |
1047.499
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| CAS # |
876296-47-8
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| Related CAS # |
Selepressin acetate
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| PubChem CID |
53330936
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
1512.1±65.0 °C at 760 mmHg
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| Flash Point |
868.3±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.545
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| LogP |
-3.83
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
21
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| Heavy Atom Count |
72
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| Complexity |
1910
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| Defined Atom Stereocenter Count |
9
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| SMILES |
C(CC[C@@H]1NC(C(NC([C@H](CC2=CC=CC=C2)NC([C@@H](N)CSSC[C@@H](C(=O)N2[C@@H](CCC2)C(=O)N[C@H](C(NCC(=O)N)=O)CCCNC(C)C)NC([C@@H](NC1=O)CC(=O)N)=O)=O)=O)[C@@H](C)CC)=O)C(N)=O
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| InChi Key |
JCVQBJTWWDYUFQ-MRUTUVJXSA-N
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| InChi Code |
InChI=1S/C46H73N13O11S2/c1-5-26(4)38-45(69)54-30(14-9-17-35(48)60)41(65)56-32(21-36(49)61)42(66)57-33(24-72-71-23-28(47)39(63)55-31(43(67)58-38)20-27-12-7-6-8-13-27)46(70)59-19-11-16-34(59)44(68)53-29(15-10-18-51-25(2)3)40(64)52-22-37(50)62/h6-8,12-13,25-26,28-34,38,51H,5,9-11,14-24,47H2,1-4H3,(H2,48,60)(H2,49,61)(H2,50,62)(H,52,64)(H,53,68)(H,54,69)(H,55,63)(H,56,65)(H,57,66)(H,58,67)/t26-,28-,29-,30-,31-,32-,33-,34-,38-/m0/s1
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| Chemical Name |
(2S)-1-[(4R,7S,10S,13S,16S,19R)-19-amino-10-(4-amino-4-oxobutyl)-7-(2-amino-2-oxoethyl)-16-benzyl-13-[(2S)-butan-2-yl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-1-oxo-5-(propan-2-ylamino)pentan-2-yl]pyrrolidine-2-carboxamide
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| Synonyms |
FE202158; FE 202158; Selepressin
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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 | 0.9539 mL | 4.7697 mL | 9.5393 mL | |
| 5 mM | 0.1908 mL | 0.9539 mL | 1.9079 mL | |
| 10 mM | 0.0954 mL | 0.4770 mL | 0.9539 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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