艾沙康唑硫酸盐 (0.006 nM–50 μM) 的 EC50 值分别为 0.001 μM、0.037 μM 和 0.024 μM，可抑制三种 T4 基因型棘阿米巴菌株（Ma、CDC:V240 和 MEEI 0184）的滋养层活性。此外，三个测试菌株 Ma、CDC:V240 和 MEEI 0184 在（100–200 μM；48 小时）表现出囊泡熄灭活性，平均最小囊泡熄灭浓度 (MCC) 分别为 167.1 μM、136.0 μM 和 187.5分别为μM[2]。

艾沙康唑硫酸盐（215 mg/kg；口服；每日 3 次，持续四天）在毛霉菌病感染的 ICR 小鼠中表现出抗 R.delemar 病毒活性[4]。

Animal Model: Neutropenic male ICR mouse model of intratracheal infection[4]
Dosage: 215 mg/kg
Administration: Oral gavage (p.o.); Three times a day for 4 days.
Result: increased the survival rate of R. delemar-infected neutropenic mice. decreased amount of fungi in the mice's brains and lungs.

[1]. Isavuconazonium sulfate: a new agent for the treatment of invasive aspergillosis and invasive mucormycosis[J]. Expert review of clinical pharmacology, 2016, 9(7): 887-897.

[2]. Evaluation of Amebicidal and Cysticidal Activities of Antifungal Drug Isavuconazonium Sulfate against Acanthamoeba T4 Strains. Pharmaceuticals (Basel). 2021 Dec 11;14(12):1294.

[3]. Isavuconazonium sulfate: a novel antifungal agent[J]. Current Fungal Infection Reports, 2015, 9: 302-313.

[4]. Isavuconazole therapy protects immunosuppressed mice from mucormycosis[J]. Antimicrobial agents and chemotherapy, 2014, 58(4): 2450-2453.

[5]. In Vitro Activity of Isavuconazole against Rasamsonia Species.Antimicrob Agents Chemother.2016 Oct 21;60(11):6890-6891.

Isavuconazonium sulfate is an azaheterocycle sulfate salt that is a prodrug for isavuconazole, an antifungal agent used for the treatment of invasive aspergillosis and invasive mucormycosis. It has a role as a prodrug, an ergosterol biosynthesis inhibitor, an EC 1.14.13.70 (sterol 14alpha-demethylase) inhibitor and an orphan drug. It is an azaheterocycle sulfate salt, a triazole antifungal drug and a conazole antifungal drug. It contains an isavuconazonium.
Isavuconazonium Sulfate is the sulfate ester form of isavuconazonium, a prodrug of the triazole antifungal agent isavuconazole, with broad-spectrum antifungal activity. Upon administration, isavuconazonium sulfate is hydrolyzed by plasma esterases to yield the active moiety isavuconazole. Isavuconazole binds to and inhibits the fungal cytochrome P450 family enzyme lanosterol 14-alpha-demethylase (CYP51), which catalyzes the demethylation of lanosterol to yield ergosterol, an important component of the fungal cell membrane. Inhibition of CYP51 leads to a decrease in fungal ergosterol production and disrupts synthesis of the fungal cell membrane, which decreases membrane integrity, increases cell membrane permeability and promotes the loss of essential intracellular elements. This results in fungal cell lysis and death.
See also: Isavuconazole (has active moiety).

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Drug Indication
Treatment of invasive aspergillosis, Treatment of mucormycosis
Treatment of Candida infections

C35H36F2N8O9S2

814.83500

814.201

C, 51.59; H, 4.45; F, 4.66; N, 13.75; O, 17.67; S, 7.87

946075-13-4

338990-84-4 (chloride);497235-79-7 (chloride HCl);742049-41-8 (cation);946075-13-4 (sulfate);

72196309

White to off-white solid powder

5.06

273.42

3

17

15

56

1290

2

S(O)([O-])(=O)=O.[C@@](C1C=C(F)C=CC=1F)(O)(CN1N=C[N+](C(C)OC(=O)N(C2N=CC=CC=2COC(=O)CNC)C)=C1)[C@H](C1SC=C(C2C=CC(C#N)=CC=2)N=1)C

LWXUIUUOMSMZKJ-KLFWAVJMSA-M

InChI=1S/C35H35F2N8O5S.H2O4S/c1-22(33-42-30(18-51-33)25-9-7-24(15-38)8-10-25)35(48,28-14-27(36)11-12-29(28)37)19-45-21-44(20-41-45)23(2)50-34(47)43(4)32-26(6-5-13-40-32)17-49-31(46)16-39-3;1-5(2,3)4/h5-14,18,20-23,39,48H,16-17,19H2,1-4H3;(H2,1,2,3,4)/q+1;/p-1/t22-,23?,35+;/m0./s1

1-((2R,3R)-3-(4-(4-cyanophenyl)thiazol-2-yl)-2-(2,5-difluorophenyl)-2-hydroxybutyl)-4-(1-((methyl(3-(((methylglycyl)oxy)methyl)pyridin-2-yl)carbamoyl)oxy)ethyl)-1H-1,2,4-triazol-4-ium hydrogen sulfate

BAL8557;BAL 8557; Isavuconazonium sulfate; BAL-8557; Cresemba.

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : 100 mg/mL ( 122.72 mM )
Water : 0.5~100 mg/mL (~0.61 mM )
Ethanol : 100 mg/mL

配方 1 中的溶解度: ≥ 2.08 mg/mL (2.55 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 20.8 mg/mL澄清DMSO储备液加入400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.08 mg/mL (2.55 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.08 mg/mL (2.55 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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配方 4 中的溶解度: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.08 mg/mL (2.55 mM)

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配方 5 中的溶解度: 100 mg/mL (122.72 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶.

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。