| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
SSTR1
Somatostatin receptor subtype 1 (SSTR1). CH 275 exhibits high selectivity for SSTR1 over other somatostatin receptor subtypes (SSTR2, SSTR3, SSTR4, SSTR5). |
|---|---|
| ln Vitro |
Neprilysin activity is activated by CH275 (100 nM), but cyclo-SRIF administration can finish this activation in vitro in primary neuron-based cell culture system, which is a mixture of cortical, striatal, and wildtype hippocampus neurons[3].
CH 275 displaces [125I]-Tyr11-SRIF-14 binding to SSTR1-expressing cells with high affinity (IC50 low nM range). It does not significantly inhibit forskolin-stimulated cAMP accumulation in SSTR2-expressing cells, confirming its SSTR1 selectivity. |
| ln Vivo |
In the App knock-in mice, CH275 (osmotic pump injection; 56 μM; two weeks) lowers the level of neprilysin/SRIF[3]. For four months, CH275 is injected directly into the Lacunosum molecular layer (Lmol) of two-month-old AppNL-GF mice. Aβ plaques are first seen in AppNL-GF mice at two months of age. However, CH275 causes a significant rise in neprilysin expression in the hippocampal region, which is accompanied by a noticeable decrease in the amount of Aβ plaques in the same area, all without having any harmful side effects[3].
In vivo studies with CH 275 demonstrate that activation of SSTR1 leads to modulation of neuronal activity and inhibition of hormone secretion in specific tissues. It has been used to investigate the role of SSTR1 in pain modulation and neuroendocrine regulation. |
| Enzyme Assay |
Competitive binding assays using membranes from CHO-K1 cells expressing human SSTR1: cell membranes are incubated with 0.1 nM [125I]-Tyr11-SRIF-14 and increasing concentrations of CH 275 in binding buffer for 60 min at 25degC. Bound radioactivity is separated by filtration and counted using a gamma counter. IC50 is calculated by nonlinear regression.
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| Cell Assay |
Functional assays for SSTR1 are performed using CHO-K1 cells stably expressing human SSTR1 and a CRE-luciferase reporter gene. Cells are treated with CH 275 for 5 hours at 37degC, and luciferase activity is measured using a luminescence plate reader to determine EC50 for Gi-mediated signaling.
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| Animal Protocol |
In vivo pharmacodynamic studies are conducted in male Sprague-Dawley rats to assess growth hormone (GH) suppression. CH 275 is administered either intravenously (0.1-1 mg/kg) or intracerebroventricularly (ICV). Blood samples are collected at baseline and post-dose for GH measurement by ELISA. Inhibition of GH release is expressed as percentage of baseline.
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| ADME/Pharmacokinetics |
CH 275 is a peptide, thus exhibits poor oral bioavailability and short plasma half-life, typical of peptides. When administered intravenously, CH 275 shows rapid clearance and limited systemic exposure. For research use, it is typically delivered via IV or ICV routes.
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| Toxicity/Toxicokinetics |
Toxicity data are limited as CH 275 is a preclinical research tool. No significant adverse effects have been reported in published studies at doses used for SSTR1 pharmacological characterization. As a somatostatin analog, potential safety concerns include effects on glucose metabolism and endocrine function.
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| References |
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| Additional Infomation |
Other information: CH 275 is widely used as a pharmacological tool to dissect the specific roles of SSTR1 in somatostatin-mediated signaling, distinct from the more clinically studied SSTR2. CH 275 is not a clinically approved drug and is intended for research use only.
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| Molecular Formula |
C74H96N14O15S2
|
|---|---|
| Molecular Weight |
1485.76885509491
|
| Exact Mass |
1470.682
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| CAS # |
174688-78-9
|
| PubChem CID |
90488765
|
| Appearance |
White to off-white solid powder
|
| LogP |
1.3
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| Hydrogen Bond Donor Count |
18
|
| Hydrogen Bond Acceptor Count |
20
|
| Rotatable Bond Count |
21
|
| Heavy Atom Count |
104
|
| Complexity |
2720
|
| Defined Atom Stereocenter Count |
13
|
| SMILES |
C([C@H]1NC([C@@H](NC([C@@]([H])(NC([C@@H](NC([C@]([H])(CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)C([C@H](O)C)NC(=O)[C@H](CC2C=CC=CC=2)NC(=O)C([C@H](O)C)NC(=O)[C@H](CC2C=CC(CNC(C)C)=CC=2)NC1=O)N)=O)CCCCN)=O)CC1C=CC=CC=1)=O)CC1C=CC=CC=1)=O)C1=CNC2C=CC=CC1=2
|
| InChi Key |
LFOPEPKKBBIGHF-RXUBGYFDSA-N
|
| InChi Code |
InChI=1S/C74H98N14O14S2/c1-43(2)77-37-50-29-27-49(28-30-50)35-59-70(97)88-64(45(4)91)73(100)86-60(34-48-22-12-7-13-23-48)71(98)87-63(44(3)90)72(99)80-52(40-89)39-79-62(74(101)102)42-104-103-41-54(76)65(92)81-56(26-16-17-31-75)66(93)82-57(32-46-18-8-5-9-19-46)67(94)83-58(33-47-20-10-6-11-21-47)68(95)85-61(69(96)84-59)36-51-38-78-55-25-15-14-24-53(51)55/h5-15,18-25,27-30,38,43-45,52,54,56-64,77-79,89-91H,16-17,26,31-37,39-42,75-76H2,1-4H3,(H,80,99)(H,81,92)(H,82,93)(H,83,94)(H,84,96)(H,85,95)(H,86,100)(H,87,98)(H,88,97)(H,101,102)/t44-,45-,52-,54+,56-,57+,58+,59-,60+,61+,62+,63-,64-/m1/s1
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| Chemical Name |
(4R,7R,10R,13S,16R,19R,22S,25S,28S,31R,34R)-34-amino-31-(4-aminobutyl)-13,25,28-tribenzyl-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-9,12,15,18,21,24,27,30,33-nonaoxo-19-[[4-[(propan-2-ylamino)methyl]phenyl]methyl]-1,2-dithia-5,8,11,14,17,20,23,26,29,32-decazacyclopentatriacontane-4-carboxylic acid
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
DMSO: 100 mg/mL (67.31 mM)
H2O: 50 mg/mL (33.65 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 | 0.6731 mL | 3.3653 mL | 6.7305 mL | |
| 5 mM | 0.1346 mL | 0.6731 mL | 1.3461 mL | |
| 10 mM | 0.0673 mL | 0.3365 mL | 0.6731 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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