TMB-8
Based on 1 publication(s) in Google Scholar
TMB-8 is a benzoate ester compound. TMB-8 blocks intracellular calcium (Ca) release, catecholamine secretion, and cholinergic/CCK-stimulated amylase release, while stimulating pancreatic hormone release and, under hyperthermia conditions, increasing cytosolic calcium and hyperthermic cell killing. TMB-8 is used in research on chemotherapy-induced painful peripheral neuropathy, human promyelocytic leukemia, and mouse breast cancer.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.0%
- CAS. Nr.: 53464-72-5
- Formel: C22H38ClNO5
- Molecular Weight:431.99
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) TMB-8
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Biologische Aktivität
Beschreibung
In Vitro
TMB-8 inhibits 1 μM Carbachol (Carbamoylcholine chloride) (HY-B1208)-stimulated amylase release, producing 57% inhibition at 10 μM, without affecting basal or 0.1 μM secretin-stimulated release[4].
TMB-8 non-selectively inhibits parasympathetic neuromuscular transmission in guinea pig ileum and contractions induced by ACh, Nicotine, DMPP, KCl, and BaCl2, with ID50 values of 3.8 × 10-6 to 14.4 × 10-6 M, but BaCl2 antagonism is competitive[7].
TMB-8 directly inhibits protein kinase C activity supported by Ca2+ and phosphatidylserine in the cytosol of partially purified bovine adrenal zona glomerulosa cells in a dose-dependent manner[10].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HL-60 human promyelocytic leukemia cells
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Concentration:10, 50, and 100 μM
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Incubation Time:4 days
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Result:At less than 50 μM, did not affect HL-60 cell proliferation.
At 100 μM, little cell proliferation was observed, but cell viability was always more than 85%.
In Vivo
TMB-8 (46 nmol; i.t.; single injection) attenuates Vincristine (HY-N0488A)-induced mechanical hypersensitivity in rats[1].
TMB-8 (46 nmol; i.t.; single injection) attenuates ddC (Zalcitabine) (HY-17392)-induced mechanical hyperalgesia in rats[1].
TMB-8 (116 nmol/10 µL; intradermal injection; single injection) attenuates ddC-induced mechanical hyperalgesia in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 250-270 g at start)[1]
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Dosage:46 nmol in 20 µL
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Administration:i.t.; single injection; at 22-28 days after paclitaxel
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Result:Reduced paclitaxel-evoked mechano-allodynia on the 4-g von Frey test and mechano-hyperalgesia on the 15-g von Frey and paw-pressure tests.
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Animal Model:Sprague-Dawley (male, 250-270 g at start)[1]
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Dosage:46 nmol in 20 µL
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Administration:i.t.; single injection; at 13-19 days after vincristine
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Result:Reduced vincristine-evoked mechano-allodynia on the 4-g von Frey test and mechano-hyperalgesia on the 15-g von Frey and paw-pressure tests.
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Animal Model:Sprague-Dawley (male, 250-270 g at start)[1]
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Dosage:46 nmol in 20 µL
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Administration:i.t.; single injection; at 8 days after ddC
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Result:Reduced ddC-evoked mechano-hyperalgesia in the paw-pressure test.
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Animal Model:Sprague-Dawley (male, 250-270 g at start)[1]
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Dosage:116 nmol/10 µL
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Administration:intradermal; single injection; at 8 days after ddC
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Result:Reduced ddC-evoked mechano-hyperalgesia in the paw-pressure test.
Chemical Information
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CAS. Nr. 53464-72-5
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Appearance Solid
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Molecular Weight 431.99
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Formel C22H38ClNO5
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Color White to off-white
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SMILES
COC1=C(C(OC)=CC(C(OCCCCCCCCN(CC)CC)=O)=C1)OC.Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 50 mg/mL (115.74 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Siau C, et al. Dysregulation of cellular calcium homeostasis in chemotherapy-evoked painful peripheral neuropathy. Anesthesia and analgesia. 2006 May;102(5):1485-90. [Content Brief]
[4]. Ikeda M, et al. Effect of an intracellular calcium antagonist (TMB-8) on carbamylcholine-induced amylase release from dispersed rat pancreatic acini. Life sciences. 1984 Feb 06;34(6):529-33. [Content Brief]
[5]. Yasuda H, et al. Stimulative effects of TMB-8 and trifluoperazine on pancreatic hormone release. Diabetes research and clinical practice. 1989 Apr 01;6(3):227-32. [Content Brief]
[6]. Wojewodzka M, et al. Calcium antagonist, TMB-8, prevents the induction of adaptive response by hydrogen peroxide or X-rays in human lymphocytes. International journal of radiation biology. 1994 Jul;66(1):99-109. [Content Brief]
[7]. Malagodi MH, et al. Pharmacological evaluation of a new Ca2+ antagonist, 8-(N,N-diethylamino)-octyl-3,4,5-trimethoxybenzoate hydrochloride (TMB-8): studies in smooth muscles. Eur J Pharmacol. 1974 Jun;27(1):25-33. [Content Brief]
[8]. Okazaki T, et al. Role of intracellular calcium ion in human promyelocytic leukemia HL-60 cell differentiation. Cancer research. 1986 Dec;46(12 Pt 1):6059-63. [Content Brief]
[9]. Kondo T, et al. Enhancement of cell killing and increase in cytosolic calcium concentration by combined treatments with hyperthermia and TMB-8 in mouse mammary carcinoma FM3A cells. Cell calcium. 1993 Oct;14(9):621-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3149 mL | 11.5743 mL | 23.1487 mL | 57.8717 mL |
| 5 mM | 0.4630 mL | 2.3149 mL | 4.6297 mL | 11.5743 mL | |
| 10 mM | 0.2315 mL | 1.1574 mL | 2.3149 mL | 5.7872 mL | |
| 15 mM | 0.1543 mL | 0.7716 mL | 1.5432 mL | 3.8581 mL | |
| 20 mM | 0.1157 mL | 0.5787 mL | 1.1574 mL | 2.8936 mL | |
| 25 mM | 0.0926 mL | 0.4630 mL | 0.9259 mL | 2.3149 mL | |
| 30 mM | 0.0772 mL | 0.3858 mL | 0.7716 mL | 1.9291 mL | |
| 40 mM | 0.0579 mL | 0.2894 mL | 0.5787 mL | 1.4468 mL | |
| 50 mM | 0.0463 mL | 0.2315 mL | 0.4630 mL | 1.1574 mL | |
| 60 mM | 0.0386 mL | 0.1929 mL | 0.3858 mL | 0.9645 mL | |
| 80 mM | 0.0289 mL | 0.1447 mL | 0.2894 mL | 0.7234 mL | |
| 100 mM | 0.0231 mL | 0.1157 mL | 0.2315 mL | 0.5787 mL |