| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Targets are the vasopressin receptors Avpr1a (V1a), Avpr1b (V1b), and Avpr2 (V2); V1a and V1b couple to Gq/11 and mobilize intracellular Ca2+, while V2 couples to Gs and stimulates cAMP; argipressin binds V1 receptors with high affinity (Kd ~1.31–1.44 nM in A7r5 smooth muscle cells and neonatal rat cardiomyocytes) and activates V1a with EC50 ~0.24 nM.
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|---|---|
| ln Vitro |
Inducing proliferation in both rodent and human beta cells, argipressin (diacetic acid) (AVP (diacetic acid)) inhibits apoptosis produced by cytokines [1].
Argipressin induces proliferation and prevents cytokine-induced apoptosis in rodent and human β-cell lines (BRIN BD11 and 1.1B4) at 10−6 M; it stimulates intracellular Ca2+ release in A7r5 rat aortic smooth muscle cells (EC50 = 5 nM) and activates V1a receptor-mediated signaling with EC50 ~0.24 nM in recombinant systems. |
| ln Vivo |
Arbopressin (diacetic acid) (AVP (diacetic acid)) (25 nmol/kg bw; intraperitoneal injection; once) significantly reduced the total AUC glucose value in mice but did not increase mouse insulin levels [1].
In rats, argipressin injected into the lateral septal nuclei (100–400 ng) induces hypertension and tachycardia, and injection into the medial amygdaloid body (150–600 ng) increases heart rate and mean arterial pressure; in mice, argipressin induces β-cell proliferation but does not increase insulin levels under the reported conditions. |
| Enzyme Assay |
Receptor-binding assays use membranes from A7r5 rat aortic smooth muscle cells, neonatal rat cardiomyocytes, or cells expressing recombinant V1a/V1b/V2 receptors, incubated with [3H]-arginine vasopressin or a suitable radioligand and graded concentrations of unlabeled argipressin; bound radioactivity is separated by filtration, and Kd and Bmax values are calculated by Scatchard analysis; selectivity is profiled across the three vasopressin receptor subtypes.
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| Cell Assay |
Cell Proliferation Assay [1]
Cell Types: Clones BRIN BD11 and 1.1B4 Cell Tested Concentrations: 10-6 M Incubation Duration: 2 hrs (hours) Experimental Results: Increased proliferation of rodent and human beta cells. Apoptosis analysis [1] Cell Types: Clones BRIN BD11 and 1.1B4 Cell Tested Concentrations: 10-6 M Incubation Duration: 2 hrs (hours) Experimental Results: Protection against cytokine-induced beta cell apoptosis. β-Cell lines (BRIN BD11, 1.1B4) or A7r5 smooth muscle cells are treated with argipressin (10−6 M) in the presence or absence of cytokines, and proliferation is measured by thymidine incorporation or cell-count assays, apoptosis by caspase-3 activity or annexin V staining, and intracellular Ca2+ mobilization by fluorometric imaging in A7r5 cells; cAMP accumulation is measured in V2-expressing cells by ELISA. |
| Animal Protocol |
Animal/Disease Models: NIH Swiss Mouse (adult; male; 12-14 weeks) [1]
Doses: 25 nmol/kg bw Route of Administration: AVP (25 nmol/kg bw; i.p.; once) Experimental Results: Overall AUC diminished ( P<0.001) glucose values, but did not increase insulin levels in mice. Rats or mice receive argipressin diacetate by intravenous, intracerebroventricular, or site-specific brain injection at doses ranging from 100 to 600 ng; cardiovascular parameters (heart rate, mean arterial pressure) are recorded by telemetry or catheterization, and in β-cell studies, mice are treated with argipressin and pancreatic tissue is analyzed for β-cell proliferation by Ki67 or BrdU incorporation and for insulin content. |
| References |
| Molecular Formula |
C46H65N15O12S2
|
|---|---|
| Exact Mass |
1143.46
|
| CAS # |
75499-44-4
|
| Related CAS # |
Argipressin;113-79-1;Argipressin acetate;129979-57-3
|
| PubChem CID |
139025970
|
| Sequence |
Cys-Tyr-Phe-Gln-Asn-Cys-Pro-Arg-Gly-NH2 (Disulfide bridge: Cys1-Cys6)CYFQNCPRG-NH2 (Disulfide bridge: Cys1-Cys6)
|
| SequenceShortening |
CYFQNCPRG-NH2 (Disulfide bridge: Cys1-Cys6)
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
1.251
|
| Hydrogen Bond Donor Count |
15
|
| Hydrogen Bond Acceptor Count |
18
|
| Rotatable Bond Count |
19
|
| Heavy Atom Count |
79
|
| Complexity |
2100
|
| Defined Atom Stereocenter Count |
8
|
| SMILES |
CC(=O)O.C1CC(N(C1)C(=O)C2CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)N)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N
|
| InChi Key |
ZHFGXNMADRRGQP-NQHFENJBSA-N
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| InChi Code |
InChI=1S/C46H65N15O12S2.C2H4O2/c47-27-22-74-75-23-33(45(73)61-17-5-9-34(61)44(72)56-28(8-4-16-53-46(51)52)39(67)54-21-37(50)65)60-43(71)32(20-36(49)64)59-40(68)29(14-15-35(48)63)55-41(69)31(18-24-6-2-1-3-7-24)58-42(70)30(57-38(27)66)19-25-10-12-26(62)13-11-25;1-2(3)4/h1-3,6-7,10-13,27-34,62H,4-5,8-9,14-23,47H2,(H2,48,63)(H2,49,64)(H2,50,65)(H,54,67)(H,55,69)(H,56,72)(H,57,66)(H,58,70)(H,59,68)(H,60,71)(H4,51,52,53);1H3,(H,3,4)/t27-,28-,29+,30+,31-,32+,33+,34-;/m0./s1
|
| Chemical Name |
acetic acid;(2S)-1-[(4S,7R,10R,13S,16R,19R)-19-amino-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-benzyl-16-[(4-hydroxyphenyl)methyl]-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]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]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.) |
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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