| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Vasopressin V1a receptor (AVPR1A). This compound is a competitive antagonist of the V1a receptor, the subtype primarily responsible for the vasoconstrictive and pressor effects of AVP. It has a high selectivity for the V1a receptor over the V2 (renal antidiuretic) and oxytocin receptors.
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|---|---|
| ln Vitro |
SKF 100273 is a highly potent antagonist of the V1a receptor. In a rat radioligand binding assay using liver V1a receptors, SKF 100273 exhibited a Ki of 1.6 nM. It is a pure antagonist, meaning it binds to the receptor and blocks AVP's action without activating it itself.
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| Enzyme Assay |
A cell-free radioligand binding assay is performed using rat liver membranes as a rich source of V1a receptors. The membranes are incubated with [3H]AVP (agonist) and varying concentrations of unlabeled SKF 100273. After incubation, bound and free radioligands are separated by filtration, and the Ki value is calculated from the competition curves.
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| Cell Assay |
For an in vitro functional assay, isolated rat aortic rings are mounted in organ baths. The rings are pre-contracted with a submaximal concentration of AVP. Then, cumulative concentrations of SKF 100273 are added to the bath, and the relaxation (reduction in tension) is measured isometrically. The concentration required to produce a 50% reversal of the AVP-induced contraction (IC50) is calculated.
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| Animal Protocol |
In vivo studies are performed in anesthetized rats. SKF 100273 is administered intravenously (i.v.), either as a bolus or constant infusion. An arterial catheter is used to monitor blood pressure. The ability of the compound to block the increase in blood pressure (pressor response) elicited by a subsequent intravenous injection of AVP is measured. A dose-response curve for the antagonist is generated.
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| ADME/Pharmacokinetics |
Not reported. As a peptide antagonist, SKF 100273 has a short plasma half-life due to rapid proteolytic degradation and renal clearance. It is therefore typically administered by intravenous infusion to achieve a stable, long-lasting blockade of V1a receptors in experimental models.
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| Toxicity/Toxicokinetics |
Not reported. As a research peptide, formal toxicology data is unavailable. Given its mechanism as a V1a antagonist, high doses could cause significant hypotension. However, in standard research protocols, it is generally well-tolerated in acute settings.
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| References | |
| Additional Infomation |
It exhibits a strong antagonistic effect on the vasopressor response of arginine vasopressin; its structure is described in the first article.
SKF 100273 is one of the most widely used selective V1a receptor antagonists. Its development was crucial for differentiating the specific functions of the V1a receptor from other vasopressin receptor subtypes (V1b, V2). It has been instrumental in studies defining the role of V1a receptors in mediating the pressor response to AVP, its involvement in myocardial ischemia, and its central nervous system effects on social behavior and stress regulation. |
| Molecular Formula |
C52H74N14O12S2
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|---|---|
| Molecular Weight |
1151.36
|
| Exact Mass |
1150.51
|
| CAS # |
73168-24-8
|
| PubChem CID |
9833460
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.5 g/cm3
|
| Index of Refraction |
1.695
|
| LogP |
3.529
|
| Hydrogen Bond Donor Count |
12
|
| Hydrogen Bond Acceptor Count |
15
|
| Rotatable Bond Count |
20
|
| Heavy Atom Count |
80
|
| Complexity |
2220
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| Defined Atom Stereocenter Count |
7
|
| SMILES |
COC1=CC=C(CC2C(NC(C(NC(C(NC(C(NC(C(N3CCCC3C(NC(C(NCC(N)=O)=O)CCCNC(N)=N)=O)=O)CSSC4(CC(N2)=O)CCCCC4)=O)CC(N)=O)=O)CCC(N)=O)=O)CC5=CC=CC=C5)=O)C=C1
|
| InChi Key |
QVQOGNOOAMQKCE-ZTYVOHGWSA-N
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| InChi Code |
InChI=1S/C52H74N14O12S2/c1-78-32-16-14-31(15-17-32)25-35-46(73)63-36(24-30-10-4-2-5-11-30)47(74)61-34(18-19-40(53)67)45(72)64-37(26-41(54)68)48(75)65-38(29-79-80-52(27-43(70)60-35)20-6-3-7-21-52)50(77)66-23-9-13-39(66)49(76)62-33(12-8-22-58-51(56)57)44(71)59-28-42(55)69/h2,4-5,10-11,14-17,33-39H,3,6-9,12-13,18-29H2,1H3,(H2,53,67)(H2,54,68)(H2,55,69)(H,59,71)(H,60,70)(H,61,74)(H,62,76)(H,63,73)(H,64,72)(H,65,75)(H4,56,57,58)/t33-,34-,35-,36-,37-,38-,39-/m0/s1
|
| Chemical Name |
(2S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-1-[(10R,13S,16S,19S,22S)-13-(2-amino-2-oxoethyl)-16-(3-amino-3-oxopropyl)-19-benzyl-22-[(4-methoxyphenyl)methyl]-12,15,18,21,24-pentaoxo-7,8-dithia-11,14,17,20,23-pentazaspiro[5.19]pentacosane-10-carbonyl]pyrrolidine-2-carboxamide
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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 | 0.8685 mL | 4.3427 mL | 8.6854 mL | |
| 5 mM | 0.1737 mL | 0.8685 mL | 1.7371 mL | |
| 10 mM | 0.0869 mL | 0.4343 mL | 0.8685 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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