レテルモビル (Synonyms: Letermovir; AIC246; MK-8228)

Name: Letermovir
Brand: MedChemExpress
SKU: HY-15233
Rating: 5.0 (19 reviews)

製品番号: HY-15233 純度: 99.96%: Data Sheet SDS COA 取扱説明書
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Technical Support

Letermovir (AIC246) is a potent inhibitor of CMV, which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.

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CAS 番号 : 917389-32-3

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 277	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 277	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$100	在庫あり	Estimated Time of Arrival: December 31
5 mg	$220	在庫あり	Estimated Time of Arrival: December 31
10 mg	$373	在庫あり	Estimated Time of Arrival: December 31
25 mg	$634	在庫あり	Estimated Time of Arrival: December 31
50 mg	$900	在庫あり	Estimated Time of Arrival: December 31
100 mg	$1284	在庫あり	Estimated Time of Arrival: December 31
500 mg	$2556	在庫あり	Estimated Time of Arrival: December 31
1 g		お問い合わせ
5 g		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 19 publication(s) in Google Scholar

Other Forms of Letermovir:

Letermovir (GMP) お問い合わせ
Letermovir (Standard) お問い合わせ

顧客検証

: Letermovir purchased from MedChemExpress. Usage Cited in: Eur J Pharm Sci. 2019 Jan 15:127:29-37. [Abstract]; Viral reporter GFP expression after inoculation and compound treatment. Infected cells treated with DMSO control, BIO, Ganciclovir (GCV) or Letermovir (LTR)

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製品説明

Letermovir (AIC246) is a potent inhibitor of CMV, which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.

Cellular Effect

Cell Line	Type	Value	Description	References
HEL	EC₅₀	0.0046 μM Compound: Letermovir	Antiviral activity against Cytomegalovirus AD-169 infected in HEL cells assessed as reduction of virus-induced cytopathogenicity Antiviral activity against Cytomegalovirus AD-169 infected in HEL cells assessed as reduction of virus-induced cytopathogenicity	[PMID: 26001344]
HEL 299	CC₅₀	63 μM Compound: AIC246	Cytotoxicity against HEL299 cells infected with human cytomegalovirus after 7 days by alamar blue assay Cytotoxicity against HEL299 cells infected with human cytomegalovirus after 7 days by alamar blue assay	[PMID: 20047911]
HEL 299	EC₅₀	0.0035 μM Compound: AIC246	Antiviral activity against human cytomegalovirus infected in HEL299 cells after 7 days by GFP-based fluorescent reduction assay Antiviral activity against human cytomegalovirus infected in HEL299 cells after 7 days by GFP-based fluorescent reduction assay	[PMID: 20047911]
HS27	CC₅₀	107 μM Compound: AIC246	Cytotoxicity against human HS27 cells infected with human cytomegalovirus after 7 days by alamar blue assay Cytotoxicity against human HS27 cells infected with human cytomegalovirus after 7 days by alamar blue assay	[PMID: 20047911]
HS27	EC₅₀	0.0056 μM Compound: AIC246	Antiviral activity against human cytomegalovirus infected in human HS27 cells after 7 days by GFP-based fluorescent reduction assay Antiviral activity against human cytomegalovirus infected in human HS27 cells after 7 days by GFP-based fluorescent reduction assay	[PMID: 20047911]
MRC5	CC₅₀	127 μM Compound: AIC246	Cytotoxicity against human MRC5 cells infected with human cytomegalovirus after 7 days by alamar blue assay Cytotoxicity against human MRC5 cells infected with human cytomegalovirus after 7 days by alamar blue assay	[PMID: 20047911]
MRC5	EC₅₀	0.0045 μM Compound: AIC246	Antiviral activity against human cytomegalovirus infected in human MRC5 cells after 7 days by GFP-based fluorescent reduction assay Antiviral activity against human cytomegalovirus infected in human MRC5 cells after 7 days by GFP-based fluorescent reduction assay	[PMID: 20047911]
NHDF	CC₅₀	91 μM Compound: AIC246	Cytotoxicity against NHDF infected with human cytomegalovirus after 7 days by alamar blue assay Cytotoxicity against NHDF infected with human cytomegalovirus after 7 days by alamar blue assay	[PMID: 20047911]

体外実験

AIC246 has consistent antiviral efficacy, and there is remarkable selectivity of AIC246 for human cytomegaloviruses^[1]. AD169 mutant strains and designated rAIC246-1 and rAIC246-2 are highly resistant to Letermovir (AIC246), with EC₅₀s of 5.6 nM, 1.24 μM, 0.37 μM, respectively. Letermovir inhibits HCMV replication through a specific antiviral mechanism that involves the viral gene product UL56. Letermovir inhibits HCMV replication in cell culture by interfering with the proper cleavage/packaging of HCMV progeny DNA^[2]. Letermovir inhibits the current gold standard GCV by more than 400-fold with respect to EC₅₀s (mean, 4.5 nM versus 2 μM) and by more than 2,000-fold with respect to EC₉₀ values (mean, 6.1 nM versus 14.5 μM)^[3]. Letermovir in conbination with anti-HCMV drugs causes additive antiviral effects, but there is no interaction between letermovir and anti-HIV drugs^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Letermovir (10-100 mg/kg/day, p.o.) leads to a dose-dependent reduction of the HCMV titer in transplanted cells compared to that of the placebo-treated control group using the mouse xenograft model^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

臨床実験

分子量

572.55

分子式

C₂₉H₂₈F₄N₄O₄

CAS 番号

917389-32-3

Appearance

Solid

Color

Off-white to yellow

SMILES

FC1=C(N=C(N2CCN(C3=CC=CC(OC)=C3)CC2)N(C4=CC(C(F)(F)F)=CC=C4OC)[C@H]5CC(O)=O)C5=CC=C1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : ≥ 100 mg/mL (174.66 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7466 mL	8.7329 mL	17.4657 mL
5 mM	0.3493 mL	1.7466 mL	3.4931 mL
10 mM	0.1747 mL	0.8733 mL	1.7466 mL

View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.37 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.96%

Select Batch:

データシート (283 KB) SDS (393 KB)

COA (251 KB) HNMR (293 KB) LCMS (93 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Marschall M, et al. In vitro evaluation of the activities of the novel anticytomegalovirus compound AIC246 (letermovir) against herpesviruses and other human pathogenic viruses. Antimicrob Agents Chemother. 2012 Feb;56(2):1135-7. [Content Brief]

[2]. Goldner T, et al. The novel anticytomegalovirus compound AIC246 (Letermovir) inhibits human cytomegalovirus replication through a specific antiviral mechanism that involves the viral terminase. J Virol. 2011 Oct;85(20):10884-93. [Content Brief]

[3]. Lischka P, et al. In vitro and in vivo activities of the novel anticytomegalovirus compound AIC246. Antimicrob Agents Chemother. 2010 Mar;54(3):1290-7. [Content Brief]

[4]. Wildum S, et al. In vitro drug combination studies of Letermovir (AIC246, MK-8228) with approved anti-human cytomegalovirus (HCMV) and anti-HIV compounds in inhibition of HCMV and HIV replication. Antimicrob Agents Chemother. 2015;59(6):3140-8. [Content Brief]

細胞実験 ^[2]	Briefly, 5×10³ AD169-infected NHDF cells/well are seeded into the wells of 30 96-well microtiter plates. The infection is allowed to proceed under the exposure of 50 nM AIC246 (10×EC₅₀) until a CPE developed in one or more of the compound-treated wells (indicative of resistant virus breakthrough). Noninfected and nontreated cells serve as controls on each plate. Mutant virus amplification is accomplwashed after cultures achieved maximum CPE by the passage of cell-free supernatant virus in the presence of 50 nM AIC246. The resultant AIC246-resistant progeny virus mutants are plaque purified three times by limiting dilutions in the presence of AIC246. The stability of resistance is tested by serially passaging plaque-purified viruses without selective pressure (8 to 10 times). MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[3]	Mice (18 to 25 g body weight) are anesthetized, and the Gelfoam sponges are implanted subcutaneously in the dorsoscapular area. After transplantation, mice are randomized and grouped in 10 animals per treatment group. Starting 4 h after transplantation, mice are treated once daily with letermovir for nine consecutive days. Drugs are applied per os by oral gavage. Total administration volume is 10 mL/kg. Mice are sacrificed after 9 days of treatment, and the Gelfoam implants are removed and digested with collagenase at 37°C. After 2 to 3 h, human cells are recovered by centrifugation and resuspended in GM. Subsequently, the isolated cell suspensions are serially diluted and mixed with uninfected NHDF indicator cells and PFU are determined by plaque assays as described above. Virus titers determined from isolated cells are given as PFU/mL. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[1]. Marschall M, et al. In vitro evaluation of the activities of the novel anticytomegalovirus compound AIC246 (letermovir) against herpesviruses and other human pathogenic viruses. Antimicrob Agents Chemother. 2012 Feb;56(2):1135-7. [Content Brief] [2]. Goldner T, et al. The novel anticytomegalovirus compound AIC246 (Letermovir) inhibits human cytomegalovirus replication through a specific antiviral mechanism that involves the viral terminase. J Virol. 2011 Oct;85(20):10884-93. [Content Brief] [3]. Lischka P, et al. In vitro and in vivo activities of the novel anticytomegalovirus compound AIC246. Antimicrob Agents Chemother. 2010 Mar;54(3):1290-7. [Content Brief] [4]. Wildum S, et al. In vitro drug combination studies of Letermovir (AIC246, MK-8228) with approved anti-human cytomegalovirus (HCMV) and anti-HIV compounds in inhibition of HCMV and HIV replication. Antimicrob Agents Chemother. 2015;59(6):3140-8. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7466 mL	8.7329 mL	17.4657 mL	43.6643 mL
	5 mM	0.3493 mL	1.7466 mL	3.4931 mL	8.7329 mL
	10 mM	0.1747 mL	0.8733 mL	1.7466 mL	4.3664 mL
	15 mM	0.1164 mL	0.5822 mL	1.1644 mL	2.9110 mL
	20 mM	0.0873 mL	0.4366 mL	0.8733 mL	2.1832 mL
	25 mM	0.0699 mL	0.3493 mL	0.6986 mL	1.7466 mL
	30 mM	0.0582 mL	0.2911 mL	0.5822 mL	1.4555 mL
	40 mM	0.0437 mL	0.2183 mL	0.4366 mL	1.0916 mL
	50 mM	0.0349 mL	0.1747 mL	0.3493 mL	0.8733 mL
	60 mM	0.0291 mL	0.1455 mL	0.2911 mL	0.7277 mL
	80 mM	0.0218 mL	0.1092 mL	0.2183 mL	0.5458 mL
	100 mM	0.0175 mL	0.0873 mL	0.1747 mL	0.4366 mL

Letermovir Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Letermovir917389-32-3AIC246 MK-8228AIC 246AIC-246MK8228MK 8228MK-8228CMVCytomegalovirusInhibitorinhibitorinhibit

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レテルモビル (Synonyms: Letermovir; AIC246; MK-8228)

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Other Forms of Letermovir:

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参考文献

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レテルモビル 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Letermovir Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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