| Size | Price | Stock | Qty |
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| 500mg |
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| Other Sizes |
| Targets |
Alpha-adrenoreceptors on the surface of platelets, which are coupled to Gq protein and initiate PLC signaling. Carbazochrome interacts with α-adrenoreceptors on platelets, promoting platelet aggregation and adhesion to form a platelet plug. The compound also reduces capillary permeability and increases capillary resistance. Carbazochrome inhibits bradykinin-induced and thrombin-induced responses.
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| ln Vitro |
In a concentration-dependent manner, carbazochrome (0.1–10 µM) suppresses the production of [3H]IP3 produced by thrombin and bradykinin [1]. The increase in permeability brought on by vasoactive drugs can be considerably reduced by adding carbochrome (0.1–1 µM) half an hour before stimulation [1].
Carbazochrome promotes hemostasis by causing the aggregation and adhesion of platelets to form a platelet plug, ceasing blood flow from an open wound. The compound interacts with α-adrenoreceptors on the surface of platelets, which are coupled to Gq protein and initiate PLC signaling. Carbazochrome also reduces capillary permeability and increases capillary resistance. It inhibits bradykinin-induced and thrombin-induced responses at concentrations of 0.1-10 µM. The compound reduces the formation of IP3 in a concentration-dependent manner by inhibiting the hydrolysis of phosphoinositides. |
| ln Vivo |
Severe pulmonary dysfunction brought on by intravenous contrast agent infusion can be prevented by Carro. In rats, radiation contrast agents can lessen lung dysfunction when carbazochrome (1–10 mg/kg) is injected intravenously [2].
In vivo, carbazochrome is used as a hemostatic agent to control capillary and parenchymal hemorrhage. It promotes blood clotting by enhancing platelet aggregation and stabilizing fragile capillaries, helping to stop bleeding from small blood vessels during trauma or surgery. Carbazochrome has been investigated for use in hemorrhoids in a mixture with troxerutin. It has been studied for its action in control of bleeding from capillaries and venules. |
| Enzyme Assay |
In vitro assays for carbazochrome involve measuring its effects on platelet aggregation using aggregometry. Platelet-rich plasma is incubated with various concentrations of carbazochrome, and aggregation is induced using agonists such as ADP or collagen. The compound's ability to promote platelet aggregation is measured. Carbazochrome also inhibits bradykinin-induced and thrombin-induced responses at 0.1-10 µM.
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| Cell Assay |
Cellular assays for carbazochrome involve treating platelets or endothelial cells with the compound and measuring platelet aggregation, adhesion, or changes in vascular permeability. The compound's effects on IP3 formation can be measured by assessing the hydrolysis of phosphoinositides. These assays demonstrate the hemostatic and capillary-stabilizing effects of carbazochrome.
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats, body weight 180-230 g [2]
Doses: 10 mg/kg Route of Administration: intravenous (iv) (iv)injection; injection 30, 60 or 90 minutes before injection of Ioxaglate (4 g I/kg, intravenous (iv) (iv)injection). Experimental Results: The increased vascular permeability of Ioxaglate was attenuated in a dose-dependent manner at doses of 1, 5 and 10 mg/kg, reaching statistical significance at doses of 5 and 10 mg/kg. In vivo animal studies for carbazochrome typically involve administration to animal models of bleeding or hemorrhage. The compound's ability to reduce bleeding time and blood loss is assessed in models of surgical trauma or injury. Carbazochrome has been studied for its action in control of bleeding from capillaries and venules. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for carbazochrome is limited. The compound is typically administered orally or parenterally for its hemostatic effects. Its metabolism and elimination pathways have not been fully characterized. The compound's hemostatic effects are rapid in onset and of short duration, requiring repeated dosing for sustained effect.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of carbazochrome have established its safety profile as a hemostatic agent. The compound is generally well tolerated at therapeutic doses. Adverse effects are rare and may include allergic reactions or gastrointestinal disturbances. The compound's safety has been demonstrated through decades of clinical use in Europe and America since the 1930s.
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| References |
[1]. Toshiaki Sendo, et al. Carbazochrome sodium sulfonate (AC-17) reverses endothelial barrier dysfunction through inhibition of phosphatidylinositol hydrolysis in cultured porcine endothelial cells. Naunyn Schmiedebergs Arch Pharmacol. 2003 Sep;368(3):175-80.
[2]. Toshiaki Sendo, et al. Carbazochrome attenuates pulmonary dysfunction induced by a radiographic contrast medium in rats. Eur J Pharmacol. 2002 Aug 23;450(2):203-8. |
| Additional Infomation |
Carbazochrome belongs to the indole class of compounds. It is functionally similar to aminourea.
See also: Carbazochrome (note moved to). Carbazochrome is a hemostatic agent that promotes clotting and prevents blood loss from open wounds. It is the semicarbazone of adrenochrome and has been used clinically since the 1930s. The compound increases capillary resistance, activates platelet factors, and promotes platelet aggregation to form a platelet plug. Carbazochrome has been investigated for use in hemorrhoids in combination with troxerutin. It remains in use in some countries as a hemostatic agent for capillary bleeding. |
| Molecular Formula |
C10H12N4O3
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|---|---|
| Molecular Weight |
236.231
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| Exact Mass |
236.09
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| CAS # |
69-81-8
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| Related CAS # |
Carbazochrome sodium sulfonate;51460-26-5
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| PubChem CID |
2557
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| Appearance |
Brown to reddish brown solid powder
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| Density |
1.6±0.1 g/cm3
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| Melting Point |
203° (dec)
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| Index of Refraction |
1.733
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| LogP |
-1.53
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
17
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| Complexity |
336
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O([H])C1([H])C2=C([H])C(=C(C([H])=C2N(C([H])([H])[H])C1([H])[H])O[H])/N=N/C(N([H])[H])=O
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| InChi Key |
SSCSSDNTQJGTJT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H12N4O3/c1-14-4-9(16)5-2-6(12-13-10(11)17)8(15)3-7(5)14/h2-3,9,15-16H,4H2,1H3,(H2,11,17)
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| Chemical Name |
(3,6-dihydroxy-1-methyl-2,3-dihydroindol-5-yl)iminourea
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| Synonyms |
AC 17; AC-17; Carbazochrome
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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 |
| 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 : ~5 mg/mL (~21.17 mM)
DMSO : ~5 mg/mL (~21.17 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 | 4.2332 mL | 21.1658 mL | 42.3316 mL | |
| 5 mM | 0.8466 mL | 4.2332 mL | 8.4663 mL | |
| 10 mM | 0.4233 mL | 2.1166 mL | 4.2332 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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