| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 1g | |||
| Other Sizes |
| Targets |
Tigloidin targets muscarinic acetylcholine receptors, which are G protein-coupled receptors that mediate the effects of the neurotransmitter acetylcholine in the central and peripheral nervous systems. As a tropane alkaloid, tigloidin is structurally similar to atropine and scopolamine, which are well-known muscarinic receptor antagonists. The compound likely binds to muscarinic receptors, inhibiting acetylcholine-mediated signaling. Depending on its specific binding affinity and selectivity, tigloidin may have effects on various physiological processes including smooth muscle contraction, glandular secretion, and heart rate.
|
|---|---|
| ln Vitro |
Tigloidin's in vitro activity is characteristic of tropane alkaloids acting at muscarinic acetylcholine receptors. In receptor binding assays, the compound would be expected to compete with radiolabeled muscarinic antagonists for binding to muscarinic receptors expressed in cell membranes or tissue homogenates. In functional assays, tigloidin would be expected to inhibit acetylcholine-induced responses such as calcium mobilization, cAMP accumulation, or smooth muscle contraction. The compound's potency and selectivity for different muscarinic receptor subtypes (M1-M5) would determine its specific pharmacological profile. Detailed in vitro data for tigloidin are limited in the available literature.
|
| ln Vivo |
Teglodine hydrobromide (20–60 mg/kg, i.p.) did not shield mice from physostigmine's fatal effects, but at doses exceeding 100 mg/kg, it shielded 80% of the subjects from the drug's deadly effects. At doses of 80–100 mg/kg, ticaclodine considerably reduced tremor-induced tremor and salivation; but, at doses of 40 mg/kg, these effects were not avoided. Ticaclodine (up to 100 mg/kg, i.p.) has no discernible effect on the drowsiness and ptosis that mice experience when given reserpine and tetrabenazine. Additionally, tigloidine administered intraperitoneally at a dose of 25–50 mg/kg did not alter a cat's behavior [1].
In vivo activity of tigloidin is characteristic of tropane alkaloids with muscarinic receptor antagonist activity. Based on its structural similarity to atropine, tigloidin would be expected to produce peripheral and central anticholinergic effects, including inhibition of salivation, bronchodilation, mydriasis (pupil dilation), and increased heart rate. At higher doses, central nervous system effects such as sedation, confusion, or hallucinations may occur. The compound's specific in vivo effects would depend on its receptor selectivity, pharmacokinetic properties, and the dose administered. Detailed in vivo data for tigloidin are limited in the available literature. |
| Enzyme Assay |
The in vitro receptor binding assay for tigloidin typically involves competition binding studies using membrane preparations from cells or tissues expressing muscarinic acetylcholine receptors. Radiolabeled muscarinic antagonist (e.g., 3H-N-methylscopolamine or 3H-quinuclidinyl benzilate) is incubated with membrane preparations and varying concentrations of tigloidin (typically 0.001 nM to 100 uM) in binding buffer (e.g., 50 mM Tris-HCl, pH 7.4) at room temperature or 37degC for 1-2 hours. Bound and free ligand are separated by filtration through glass fiber filters, and radioactivity is measured by scintillation counting. The inhibition constant (Ki) is calculated from IC50 values. Non-specific binding is determined in the presence of excess unlabeled atropine. Selectivity for muscarinic receptor subtypes can be assessed using membranes from cells expressing individual subtypes.
|
| Cell Assay |
In vitro cellular assays for tigloidin are conducted using cell lines expressing muscarinic acetylcholine receptors. Cells are seeded in 96-well plates and treated with varying concentrations of tigloidin (typically 0.001 nM to 100 uM) in the presence or absence of a muscarinic agonist such as carbachol or acetylcholine. Receptor activation is assessed by measuring intracellular calcium mobilization using fluorescent calcium indicators (e.g., Fluo-4), or by measuring inositol phosphate accumulation or cAMP levels depending on the receptor subtype. The antagonist potency is determined by assessing the compound's ability to inhibit agonist-induced responses. Cell viability is monitored to ensure that observed effects are not due to cytotoxicity.
|
| Animal Protocol |
In vivo animal studies for tigloidin typically involve administration to rodents to assess its anticholinergic effects. The compound is administered by intravenous, intraperitoneal, or subcutaneous injection at doses ranging from 0.01-10 mg/kg. Classic pharmacological assays for anticholinergic activity include measurement of mydriasis (pupil dilation) using a pupilometer, inhibition of carbachol-induced salivation, inhibition of acetylcholine-induced bronchoconstriction, and measurement of heart rate changes by ECG. Behavioral tests may be performed to assess central nervous system effects. The compound's effects on gastrointestinal motility may also be assessed. Specific protocols depend on the research question and the effects being studied.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of tigloidin are characteristic of tropane alkaloids. As a small molecule alkaloid, it is expected to have good oral bioavailability and the ability to cross the blood-brain barrier. The compound's pharmacokinetic profile would include absorption, distribution, metabolism, and excretion parameters consistent with other tropane alkaloids. However, detailed ADME parameters for tigloidin specifically are not extensively documented in the available literature. The compound should be stored under appropriate conditions as recommended by the supplier.
|
| Toxicity/Toxicokinetics |
Tigloidin is a tropane alkaloid and, like other compounds in this class, can be toxic at high doses. Tropane alkaloids act as anticholinergic agents, and overdose can cause symptoms including dry mouth, blurred vision, tachycardia, urinary retention, confusion, hallucinations, and in severe cases, seizures and respiratory depression. The compound is for research use only and is not intended for human therapeutic use. Standard safety precautions should be followed when handling the compound in a laboratory setting. No specific LD50 values have been reported.
|
| References | |
| Additional Infomation |
Reports indicate that datura contains tropical sulfide, and relevant data is available for reference.
Tigloidin (CAS 495-83-0) is a tropane alkaloid structurally related to atropine, scopolamine, and other tropane alkaloids found in plants of the Solanaceae family. As a tropane alkaloid, tigloidin is expected to act as a muscarinic acetylcholine receptor antagonist, producing anticholinergic effects. The compound is used in pharmacological research to study cholinergic signaling and receptor pharmacology. It is available for research purposes only. Detailed information about this specific compound, including its receptor binding affinity, selectivity, and specific research applications, is limited in the publicly available literature. |
| Molecular Formula |
C13H21NO2
|
|---|---|
| Molecular Weight |
223.31134
|
| Exact Mass |
223.157
|
| CAS # |
495-83-0
|
| PubChem CID |
12444363
|
| Appearance |
Light yellow to yellow liquid
|
| Density |
1.06g/cm3
|
| Boiling Point |
290.2ºC at 760 mmHg
|
| Flash Point |
99.9ºC
|
| Vapour Pressure |
0.0021mmHg at 25°C
|
| Index of Refraction |
1.514
|
| LogP |
2.058
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
16
|
| Complexity |
297
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
C/C=C(C)/C(O[C@H]1C[C@@H](N2C)CC[C@@H]2C1)=O
|
| InChi Key |
UVHGSMZRSVGWDJ-ZCFDAEMWSA-N
|
| InChi Code |
InChI=1S/C13H21NO2/c1-4-9(2)13(15)16-12-7-10-5-6-11(8-12)14(10)3/h4,10-12H,5-8H2,1-3H3/b9-4+/t10-,11+,12?
|
| Chemical Name |
[(1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] (E)-2-methylbut-2-enoate
|
| 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 | 4.4781 mL | 22.3904 mL | 44.7808 mL | |
| 5 mM | 0.8956 mL | 4.4781 mL | 8.9562 mL | |
| 10 mM | 0.4478 mL | 2.2390 mL | 4.4781 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
