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1mg |
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5mg |
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CYN154806 (CYN-154806) is a cyclic octapeptide acting as a somatostatin sst2 receptor antagonist,with pIC50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively.
ln Vitro |
In CHO-K1 cells expressing the human sst2 receptor, CYN 154806 prevents the rise in extracellular acidification (EAR) brought on by SRIF (pKB 7.92). Additionally, CYN 154806 prevents the SRIF-induced rise in [35S]-GTPγS binding in the membranes of CHO-K1 cells that express the rat sst2(a) and rat sst2(b) receptors (pKB 7.81, 7.68, and 7.96) in addition to the human sst2 receptor [2].
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ln Vivo |
The decreased acid response to carbachol (CCh) (30 μg/kg) in M4 KO mice is dose-dependently and significantly reversed by CYN 154806 (0.1 mg/kg; i.p.; 20 min before administration of CCh). , but is unable to restore the M3 KO mice's reduced acid response to CCh [3].
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References |
[1]. Bass RT, et al. Identification and characterization of novel somatostatin antagonists. Mol Pharmacol. 1996 Oct;50(4):709-15.
[2]. Feniuk W, et al. Selective somatostatin sst(2) receptor blockade with the novel cyclic octapeptide, CYN-154806. Neuropharmacology. 2000 Jun 8;39(8):1443-50. [3]. Takeuchi K, et al. Activation of Muscarinic Acetylcholine Receptor Subtype 4 Is Essential for Cholinergic Stimulation of Gastric Acid Secretion: Relation to D Cell/Somatostatin. Front Pharmacol. 2016 Aug 30;7:278. |
Molecular Formula |
C56H68N12O14S2
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Molecular Weight |
1197.34112
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CAS # |
183658-72-2
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Related CAS # |
CYN 154806 TFA;2828432-46-6
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SMILES |
NCCCC[C@H]1C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@H](C(N[C@H](CC2=CC=C(O)C=C2)C(N)=O)=O)CSSC[C@@H](NC([C@@H](NC(C)=O)CC2=CC=C(N([O-])=O)C=C2)=O)C(=O)N[C@@H](CC2=CC=C(O)C=C2)C(=O)N[C@H](CC2C3=CC=CC=C3NC=2)C(=O)N1
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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) |
H2O : ~12.5 mg/mL (~10.44 mM)
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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 | 0.8352 mL | 4.1759 mL | 8.3518 mL | |
5 mM | 0.1670 mL | 0.8352 mL | 1.6704 mL | |
10 mM | 0.0835 mL | 0.4176 mL | 0.8352 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.