4,4′-STILBENEDICARBOXAMIDINE, DIHYDROCHLORIDE

Modify Date: 2024-04-05 18:14:51

4,4′-STILBENEDICARBOXAMIDINE, DIHYDROCHLORIDE Structure
4,4′-STILBENEDICARBOXAMIDINE, DIHYDROCHLORIDE structure
Common Name 4,4′-STILBENEDICARBOXAMIDINE, DIHYDROCHLORIDE
CAS Number 6935-63-3 Molecular Weight 337.25
Density N/A Boiling Point 456.4ºC at 760 mmHg
Molecular Formula C16H18Cl2N4 Melting Point N/A
MSDS N/A Flash Point 229.8ºC

 Use of 4,4′-STILBENEDICARBOXAMIDINE, DIHYDROCHLORIDE


Stilbamidine dihydrochloride is a diamidine compound derived from Stilbene and used chiefly in the form of its crystalline isethionate salt in treating various fungal infections.

 Names

Name trans-stilbene-4,4'-dicarboxamidine, dihydrochloride

  Biological Activity

Description Stilbamidine dihydrochloride is a diamidine compound derived from Stilbene and used chiefly in the form of its crystalline isethionate salt in treating various fungal infections.
Related Catalog
In Vitro 高亲和力 pentamidine 转运蛋白 (HAPT1) 被 Propamidine 抑制,但对 Stilbamidine dihydrochloride 仅显示低亲和力。相反,腺苷敏感的 pentamidine 转运蛋白 (ASPT1) 会被二盐酸二苯巴脒和 Propamidine 强烈抑制。在不同浓度的腺苷 (IC50=1.2 μM) 或 Melarsen oxide (IC50=0.7 μM) 存在下测定 [3H]pentamidine 摄取=0.7 μM),以及存在 250 μM 腺苷和增加浓度的次黄嘌呤、Propamidine (IC50=6.1 μM) 和 Stilbamidine dihydrochloride (IC50=110 μM)[1]。两种二脒化合物,Stilbamidine dihydrochloride 和 Pentamidine 用于治疗多发性骨髓瘤,这种疾病经常发生血清球蛋白含量增加[2]。
References

[1]. De Koning HP. Uptake of pentamidine in Trypanosoma brucei brucei is mediated by three distinct transporters: implications for cross-resistance with arsenicals. Mol Pharmacol. 2001 Mar;59(3):586-92.  

[2]. BREWER AE.et al. Multiple myeloma treated with stilbamidine and pentamidine. Br Med J. 1948 Dec 4;2(4587):978-82.  

 Chemical & Physical Properties

Boiling Point 456.4ºC at 760 mmHg
Molecular Formula C16H18Cl2N4
Molecular Weight 337.25
Flash Point 229.8ºC
Exact Mass 300.11400
PSA 99.74000
LogP 4.82720

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
WJ5340000
CHEMICAL NAME :
4,4'-Stilbenedicarboxamidine, dihydrochloride
CAS REGISTRY NUMBER :
6935-63-3
LAST UPDATED :
199712
DATA ITEMS CITED :
4
MOLECULAR FORMULA :
C16-H16-N4.2Cl-H
MOLECULAR WEIGHT :
337.28
WISWESSER LINE NOTATION :
MUYZR D1U1R DYZUM &GH 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
91 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes
REFERENCE :
ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 2,581,1952
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
180 mg/kg
TOXIC EFFECTS :
Brain and Coverings - recordings from specific areas of CNS Lungs, Thorax, or Respiration - other changes Nutritional and Gross Metabolic - body temperature decrease
REFERENCE :
ATMPA2 Annals of Tropical Medicine and Parasitology. (Grune & Stratton, Inc., POB 6280, Duluth, MN 55806) V.1- 1907- Volume(issue)/page/year: 37,1,1943
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
18900 ug/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes
REFERENCE :
ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 2,581,1952 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
360 mg/kg/10D-I
TOXIC EFFECTS :
Vascular - regional or general arteriolar or venous dilation Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
ATMPA2 Annals of Tropical Medicine and Parasitology. (Grune & Stratton, Inc., POB 6280, Duluth, MN 55806) V.1- 1907- Volume(issue)/page/year: 37,1,1943