| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
The human endothelin-1 (1-31) (100 pM-100 nM; 24 h) stimulates the growth of mesangial cells [2]. Human Endothelin-1 (1-31) at 100 nM for 0–10 min
|
|---|---|
| ln Vivo |
Mesocolic artery contraction is induced by ET-1(1-31) (100 nM; single dosage). Age may cause contractions to worsen and may be mediated by ETA receptors. The state of chronic diabetes at the moment
|
| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: Human mesangial cells Tested Concentrations: 100 pM-100 nM Incubation Duration: 24 h Experimental Results: Causes[3H] -increased thymidine incorporation) induces ERK activation in human mesangial cells [2]. Enters cells in a concentration-dependent manner. Western Blot Analysis[2] Cell Types: Human Mesangial Cells Tested Concentrations: 100 nM Incubation Duration: 0, 5, 10, 15 and 30 minutes Experimental Results: ERK activity rapidly increased 2.45-fold at 5 minutes and reached a peak at 10 minutes . The activity of both ERKs diminished rapidly and returned to baseline control values 30 min after stimulation. |
| Animal Protocol |
Animal/Disease Models: ICR mouse, streptozotocin-induced diabetes model [1]
Doses: 100 nM Route of Administration: in organ bath, single dose Experimental Results: in 1 week control (but not in non-diabetic In the group, the induced contraction and contractile response of female mice were Dramatically stronger than that of male mice, and there were no significant differences between age-matched controls and diabetic mice in either male or female mice. In the 8-week group, compared with the corresponding The contractions in all mice increased or tended to increase compared to the 1-week group. Although in male mice, there was no difference in this contraction between the control and diabetic groups, the contractions in diabetic female mice were Dramatically greater than those in the control group of female mice, and contractions in female diabetic mice were Dramatically greater than in male diabetic mice. ETA receptor inhibitors inhibited contractions. |
| References |
| Molecular Formula |
C162H236N38O47S5
|
|---|---|
| Molecular Weight |
3628.15867233276
|
| Exact Mass |
3625.584
|
| CAS # |
133972-52-8
|
| Related CAS # |
Endothelin-1 (1-31) (Human) TFA;Endothelin-1 (1-31) (Human) acetate
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.3±0.1 g/cm3
|
| Index of Refraction |
1.570
|
| LogP |
0.04
|
| SMILES |
S1C([H])([H])[C@@]([H])(C(N([H])[C@@]([H])(C([H])([H])C2=C([H])N([H])C([H])=N2)C(N([H])[C@@]([H])(C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])C(N([H])[C@@]([H])(C([H])([H])C(=O)O[H])C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@@]([H])(C([H])([H])C2=C([H])N([H])C3=C([H])C([H])=C([H])C([H])=C23)C(N([H])[C@@]([H])(C([H])(C([H])([H])[H])C([H])([H])[H])C(N([H])[C@@]([H])(C([H])([H])C(N([H])[H])=O)C(N([H])[C@@]([H])([C@@]([H])(C([H])([H])[H])O[H])C(N2C([H])([H])C([H])([H])C([H])([H])[C@@]2([H])C(N([H])[C@]([H])(C(N([H])[C@@]([H])(C([H])([H])C2=C([H])N([H])C([H])=N2)C(N([H])[C@@]([H])(C([H])(C([H])([H])[H])C([H])([H])[H])C(N([H])[C@@]([H])(C([H])(C([H])([H])[H])C([H])([H])[H])C(N2C([H])([H])C([H])([H])C([H])([H])[C@@]2([H])C(N([H])[C@]([H])(C(=O)O[H])C([H])([H])C2C([H])=C([H])C(=C([H])C=2[H])O[H])=O)=O)=O)=O)=O)C([H])([H])C([H])([H])C(=O)O[H])=O)=O)=O)=O)=O)=O)[C@@]([H])(C([H])([H])[H])C([H])([H])C([H])([H])[H])=O)[C@@]([H])(C([H])([H])[H])C([H])([H])C([H])([H])[H])=O)=O)=O)=O)N([H])C([C@]([H])(C([H])([H])C2C([H])=C([H])C([H])=C([H])C=2[H])N([H])C([C@]([H])(C([H])([H])C2C([H])=C([H])C(=C([H])C=2[H])O[H])N([H])C([C@]([H])(C([H])(C([H])([H])[H])C([H])([H])[H])N([H])C([C@]2([H])C([H])([H])SSC([H])([H])[C@@]([H])(C(N([H])[C@@]([H])(C([H])([H])O[H])C(N([H])[C@@]([H])(C([H])([H])O[H])C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@@]([H])(C([H])([H])C(=O)O[H])C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N2[H])=O)C([H])([H])C([H])([H])C(=O)O[H])=O)C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])[H])=O)=O)C([H])([H])C([H])([H])SC([H])([H])[H])=O)C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])=O)=O)=O)N([H])C([C@]([H])(C([H])([H])O[H])N([H])C([C@]([H])(C([H])([H])S1)N([H])[H])=O)=O)=O)=O)=O)=O
|
| InChi Key |
JKSRICZEYPPRFI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C162H236N38O47S5/c1-19-83(15)129(158(242)183-105(59-89-65-168-96-33-25-24-32-94(89)96)143(227)192-125(79(7)8)156(240)184-108(62-120(165)207)145(229)198-131(85(17)204)161(245)200-52-29-35-118(200)153(237)174-99(46-48-122(210)211)134(218)178-107(61-91-67-167-76-170-91)144(228)193-127(81(11)12)157(241)195-128(82(13)14)160(244)199-51-28-36-119(199)154(238)185-111(162(246)247)58-88-39-43-93(206)44-40-88)197-159(243)130(84(16)20-2)196-146(230)110(64-124(214)215)181-138(222)102(55-78(5)6)175-141(225)106(60-90-66-166-75-169-90)179-150(234)115-72-250-249-71-95(164)132(216)186-112(68-201)149(233)191-116-73-251-252-74-117(152(236)194-126(80(9)10)155(239)182-104(57-87-37-41-92(205)42-38-87)139(223)177-103(140(224)190-115)56-86-30-22-21-23-31-86)189-135(219)98(45-47-121(208)209)172-133(217)97(34-26-27-50-163)171-142(226)109(63-123(212)213)180-136(220)100(49-53-248-18)173-137(221)101(54-77(3)4)176-147(231)113(69-202)187-148(232)114(70-203)188-151(116)235/h21-25,30-33,37-44,65-67,75-85,95,97-119,125-131,168,201-206H,19-20,26-29,34-36,45-64,68-74,163-164H2,1-18H3,(H2,165,207)(H,166,169)(H,167,170)(H,171,226)(H,172,217)(H,173,221)(H,174,237)(H,175,225)(H,176,231)(H,177,223)(H,178,218)(H,179,234)(H,180,220)(H,181,222)(H,182,239)(H,183,242)(H,184,240)(H,185,238)(H,186,216)(H,187,232)(H,188,235)(H,189,219)(H,190,224)(H,191,233)(H,192,227)(H,193,228)(H,194,236)(H,195,241)(H,196,230)(H,197,243)(H,198,229)(H,208,209)(H,210,211)(H,212,213)(H,214,215)(H,246,247)
|
| Chemical Name |
4-[[1-[2-[[4-amino-2-[[2-[[2-[[2-[[2-[[2-[[2-[[2-[[31-amino-7-(4-aminobutyl)-39-benzyl-4-(2-carboxyethyl)-10-(carboxymethyl)-19,22,28-tris(hydroxymethyl)-42-[(4-hydroxyphenyl)methyl]-16-(2-methylpropyl)-13-(2-methylsulfanylethyl)-3,6,9,12,15,18,21,24,27,30,38,41,44,47-tetradecaoxo-45-propan-2-yl-33,34,49,50-tetrathia-2,5,8,11,14,17,20,23,26,29,37,40,43,46-tetradecazabicyclo[23.22.4]henpentacontane-36-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-3-carboxypropanoyl]amino]-3-methylpentanoyl]amino]-3-methylpentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-methylbutanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-[[1-[[1-[[1-[2-[[1-carboxy-2-(4-hydroxyphenyl)ethyl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
|
| 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 |
| 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) |
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
|
|---|---|
| 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 | 0.2756 mL | 1.3781 mL | 2.7562 mL | |
| 5 mM | 0.0551 mL | 0.2756 mL | 0.5512 mL | |
| 10 mM | 0.0276 mL | 0.1378 mL | 0.2756 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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