BIM 23127 |
Catalog No.GC11620
One-Click Copy Product Info
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BIM 23127 is a highly selective agonist for somatostatin receptor subtype 2 (SSTR2) with a Ki value of 20.9nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 160161-61-5
Sample solution is provided at 25 µL, 10mM.
BIM 23127 is a highly selective agonist for somatostatin receptor subtype 2 (SSTR2) with a Ki value of 20.9nM[1]. By binding to SSTR2, BIM 23127 inhibits cAMP accumulation and modulates downstream effectors, thereby exerting its biological activities[2]. BIM 23127 is used to investigate the role of somatostatin in regulating hormone secretion, and cell proliferation[3]. BIM 23127 has also demonstrated potential in suppressing tumor and cancer cell proliferation[4].
In vitro, pretreatment of RAW-Blue macrophages, PANC-1 cells, and SW-620 cells with BIM 23127 (12.5μg/mL) for 1 hour, followed by stimulation with the CB1 receptor agonist AM-404 (2.57μg/mL), significantly inhibited Neu-1 sialidase activity and blocked CB1 receptor-mediated activation of the NF-κB signaling pathway[5]. In HTC-WT cells (rat hepatoma cells), pretreatment with BIM 23127 (333μg/mL) for 30 minutes, followed by stimulation with insulin (100nM) or bombesin, markedly suppressed insulin-induced Neu1 sialidase activity and inhibited neuromedin B receptor (NMBR)-mediated insulin receptor signaling pathway activation[6].
In vivo, intracerebroventricular pretreatment with BIM 23127 (3nmol/animal) 30 minutes prior to bombesin (0.03nmol/animal) administration significantly attenuated bombesin-induced shortening of the urinary interval in rats and blocked bombesin receptor subtype-1 (BB1)-mediated hyperreflexia of the mitcurition reflex[7]. Intraperitoneal pretreatment with BIM 23127 (16–64nmol/kg) 15 minutes prior to behavioral testing significantly impaired memory acquisition in a mouse inhibitory avoidance learning task, with the most pronounced effect observed at a dose of 32nmol/kg[8].
References:
[1] Ladenheim EE, Taylor JE, Coy DH, et al. Blockade of feeding inhibition by neuromedin B using a selective receptor antagonist. Eur J Pharmacol. 1994 Dec 12;271(1):R7-9.
[2] Herold CL, Behm DJ, Buckley PT, et al. The neuromedin B receptor antagonist, BIM-23127, is a potent antagonist at human and rat urotensin-II receptors. Br J Pharmacol. 2003 May;139(2):203-7.
[3] Ladenheim EE, Taylor JE, Coy DH, et al. Caudal hindbrain neuromedin B-preferring receptors participate in the control of food intake. Am J Physiol. 1997 Jan;272(1 Pt 2):R433-7.
[4] Jaeger M, Ghisleni EC, Fratini L, et al. Viability of D283 medulloblastoma cells treated with a histone deacetylase inhibitor combined with bombesin receptor antagonists. Childs Nerv Syst. 2016 Jan;32(1):61-4.
[5] Bunsick DA, Matsukubo J, Aldbai R, et al. Functional Selectivity of Cannabinoid Type 1 G Protein-Coupled Receptor Agonists in Transactivating Glycosylated Receptors on Cancer Cells to Induce Epithelial-Mesenchymal Transition Metastatic Phenotype. Cells. 2024 Mar 8;13(6):480.
[6] Alghamdi F, Guo M, Abdulkhalek S, et al. A novel insulin receptor-signaling platform and its link to insulin resistance and type 2 diabetes. Cell Signal. 2014 Jun;26(6):1355-68.
[7] Shimizu T, Shimizu S, Higashi Y, et al. A Stress-Related Peptide Bombesin Centrally Induces Frequent Urination through Brain Bombesin Receptor Types 1 and 2 in the Rat. J Pharmacol Exp Ther. 2016 Mar;356(3):693-701.
[8] Santo-Yamada Y, Yamada K, Wada E, et al. Blockade of bombesin-like peptide receptors impairs inhibitory avoidance learning in mice. Neurosci Lett. 2003 Apr 3;340(1):65-8.
| Cell experiment [1]: | |
Cell lines | DAOY and D283 cells (human medulloblastoma cell lines) |
Preparation Method | Cells were maintained in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum (FBS). Cells were treated with the NMBR antagonist BIM 23127 (1nM–10µM), either alone or in combination with the anti-EGFR monoclonal antibody cetuximab (1 or 10µg/mL), for 48 hours. |
Reaction Conditions | 1nM–10µM; 48h |
Applications | BIM 23127 alone did not significantly affect cell death/proliferation in either DAOY or D283 cells. However, BIM 23127 combined with a low, ineffective dose of cetuximab (1µg/mL) significantly reduced the number of DAOY cells. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Rats were anesthetized with urethane (1.0-1.2g/kg; i.p.) and implanted with intracerebroventricular (i.c.v.) cannulas targeting the right lateral ventricle. BIM 23127 (3nmol/animal) or vehicle (5μl saline) was administered i.c.v. 30 minutes prior to bombesin (0.03nmol/animal; i.c.v.). Continuous cystometrograms (CMG) were recorded to assess bladder activity. |
Dosage form | 3nmol/animal; i.c.v. |
Applications | Pretreatment with BIM 23127 significantly attenuated bombesin-induced shortening of intercontraction intervals (ICI), indicating blockade of central neuromedin B receptors (BB1) reduced stress-related bladder overactivity without affecting basal voiding parameters. |
| Cas No. | 160161-61-5 | SDF | |
| Canonical SMILES | CC([C@@]1([H])/C(O)=N/[C@@](/C(O)=N/[C@](C(O)=N)([H])CC2=CC3=CC=CC=C3C=C2)([H])CSSC[C@@](/N=C(O)/[C@@](N)([H])CC4=CC5=CC=CC=C5C=C4)([H])/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/1)([H])CCCN)([H])CC6=CNC7=CC=CC=C67)([H])CC8=CC=C(O)C=C8)C | ||
| Formula | C62H71N11O9S2 | M.Wt | 1178.43 |
| Solubility | Soluble to 2 mg/ml in 20% acetonitrile | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 848.6 μL | 4.2429 mL | 8.4859 mL |
| 5 mM | 169.7 μL | 848.6 μL | 1.6972 mL |
| 10 mM | 84.9 μL | 424.3 μL | 848.6 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)