![d[Cha4]-AVP](/upload/1124/V74532.png)
| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
Ki: 1.2 nM (vasopressin V1B receptor), 151 nM (vasopressin V1A receptor), 240 nM (Oxytocin receptor), 750 nM (vasopressin V2 receptor)[1]
Vasopressin V1b receptor. d[Cha4]-AVP is a potent and selective agonist of the vasopressin V1b receptor. It has a Ki of 1.2 nM for the human V1b receptor and shows greater selectivity for V1b over V1a, V2, and oxytocin receptors. By activating the V1b receptor, it stimulates ACTH and corticosterone secretion. |
|---|---|
| ln Vitro |
d[Cha4]-AVP has pKi values of 7.68 and 9.68, respectively, for its binding to human oxytocin receptors and hV1b receptors[2]. d[Cha4]-AVP has a pEC50 value of 10.05 and increases [Ca2+]i in hV1b-CHO cells. At hV1a and hV2 receptors, d[Cha4]-AVP exhibits pEC50 values of 6.53 and 5.92, respectively, and functions as a weak antagonist at hOT receptors (pKB=6.31)[2].
d[Cha4]-AVP is a potent and selective V1b receptor agonist with a Ki of 1.2 nM. It shows Ki values of 151 nM for V1a, and even higher values for oxytocin and V2 receptors. By selectively activating the V1b receptor, it stimulates ACTH and corticosterone secretion in vitro. |
| ln Vivo |
In vivo, d[Cha4]-AVP stimulates ACTH and corticosterone secretion, demonstrating its ability to activate the hypothalamic-pituitary-adrenal (HPA) axis. It exhibits negligible vasopressor activity in vivo, consistent with its selectivity for the V1b receptor over the V1a receptor. This makes it a valuable tool for studying V1b receptor function without significant cardiovascular effects.
|
| Enzyme Assay |
In vitro receptor binding assays are used to characterize d[Cha4]-AVP as a V1b receptor agonist. Radioligand binding assays are performed using membranes from cells expressing the human V1b, V1a, V2, and oxytocin receptors to determine its binding affinities and selectivity. It has a Ki of 1.2 nM for V1b and 151 nM for V1a.
|
| Cell Assay |
Cellular assays for d[Cha4]-AVP involve treating V1b receptor-expressing cells with the compound and measuring receptor activation. Functional readouts include intracellular calcium mobilization or downstream signaling pathways. These assays confirm the compound's agonistic activity and potency at the V1b receptor.
|
| Animal Protocol |
In vivo studies with d[Cha4]-AVP are performed in animal models to investigate V1b receptor function in the HPA axis. The compound is administered via injection, and its effects on ACTH and corticosterone secretion are measured. Its negligible vasopressor activity confirms its selectivity for V1b over V1a in vivo.
|
| ADME/Pharmacokinetics |
d[Cha4]-AVP is a peptide with molecular formula C50H71N13O11S2 and molecular weight of 1094.31. It is soluble in water (90 mg/mL). As a peptide agonist, its pharmacokinetic properties would be characteristic of this class, with a short half-life. The compound should be stored under recommended conditions.
|
| Toxicity/Toxicokinetics |
No specific toxicity data is available for d[Cha4]-AVP. As a V1b receptor agonist, its safety profile would be an important consideration. Potential toxicities could be related to its effects on the HPA axis and stress responses. Standard preclinical safety studies would be required to evaluate its safety for potential therapeutic applications.
|
| References |
|
| Additional Infomation |
d[Cha4]-AVP (CAS#: 500170-27-4) is a potent and selective vasopressin V1b receptor agonist with a Ki of 1.2 nM for the human V1b receptor. It shows high selectivity over V1a, V2, and oxytocin receptors. It stimulates ACTH and corticosterone secretion and exhibits negligible vasopressor activity in vivo. It has a molecular formula of C50H71N13O11S2 and a molecular weight of 1094.31.
|
| Molecular Formula |
C50H71N13O11S2
|
|---|---|
| Molecular Weight |
1094.31
|
| Exact Mass |
1095.5
|
| CAS # |
500170-27-4
|
| Related CAS # |
d[Cha4]-AVP TFA
|
| PubChem CID |
44419028
|
| Appearance |
White to off-white solid powder
|
| LogP |
3.303
|
| Hydrogen Bond Donor Count |
12
|
| Hydrogen Bond Acceptor Count |
14
|
| Rotatable Bond Count |
18
|
| Heavy Atom Count |
76
|
| Complexity |
2050
|
| Defined Atom Stereocenter Count |
7
|
| SMILES |
C1CCC(CC1)C[C@H]2C(=O)N[C@H](C(=O)N[C@@H](CSSCCC(=O)N[C@H](C(=O)N[C@H](C(=O)N2)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)C(=O)N5CCC[C@H]5C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(=O)N)CC(=O)N
|
| InChi Key |
ZKYCVZNKBXGNEK-ZTYVOHGWSA-N
|
| InChi Code |
InChI=1S/C50H71N13O11S2/c51-40(65)26-37-47(72)62-38(49(74)63-21-8-14-39(63)48(73)58-33(13-7-20-55-50(53)54)43(68)56-27-41(52)66)28-76-75-22-19-42(67)57-34(25-31-15-17-32(64)18-16-31)44(69)59-35(23-29-9-3-1-4-10-29)45(70)60-36(46(71)61-37)24-30-11-5-2-6-12-30/h1,3-4,9-10,15-18,30,33-39,64H,2,5-8,11-14,19-28H2,(H2,51,65)(H2,52,66)(H,56,68)(H,57,67)(H,58,73)(H,59,69)(H,60,70)(H,61,71)(H,62,72)(H4,53,54,55)/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-[(4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-13-benzyl-10-(cyclohexylmethyl)-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide
|
| 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, avoid exposure to moisture. |
| 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) |
H2O: 100 mg/mL (91.38 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
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 | 0.9138 mL | 4.5691 mL | 9.1382 mL | |
| 5 mM | 0.1828 mL | 0.9138 mL | 1.8276 mL | |
| 10 mM | 0.0914 mL | 0.4569 mL | 0.9138 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
