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Nosiheptide 56377-79-8 GlpBio

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2024年11月3日发(作者:威聪)

Peptides, Inhibitors, Agonists

Product Data Sheet

Product Name:

Cat. No.:

Nosiheptide

GC38117

Chemical Properties

Cas No.

Chemical

Name

Canonical

SMILES

Formula

Solubility

General tips

Shipping

Condition

56377-79-8

N/A

OC1=C(C2=NC(C(NC(C(N)=O)=C)=O)=CS2)N=C(C3=CSC(C4NC(C5=CSC(C(CC(C(OCC6=C7C(C)=C(

NC7=CC=C6)C(SC4)=O)=O)O)NC(C8=CSC(/C(NC(C(C(O)C)NC(C9=CSC%10=N9)=O)=O)=CC)=N8)=

O)=N5)=O)=N3)C%10=C1

C

51

H

43

N

13

O

12

S

6

Soluble in DMSO

Storage

1222.36

Store at -20°C

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath

for a solution can be stored below -20℃ for several months.

Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon

request.

Structure

Background

Nosiheptide (Multhiomycin), a thiopeptide antibiotic produced by Streptomyces actuosus, inhibits bacterial protein

Caution: Producthasnot been fully validated for medical applications. For research use only.

Tel: (626) 353-8530 Fax: (626) 353-8530 E-mail: tech@

Address: 10292 Central Ave. #205, Montclair, CA, USA

Peptides, Inhibitors, Agonists

Product Data Sheet

synthesis and bears a unique indole side ring system and regiospecific hydroxyl groups on the characteristic

macrocyclic core. Nosiheptide has been widely used as a feed additive for animal growth[1][2].

Nosiheptide exhibits extremely potent activity against all contemporary Staphylococcus aureus strains tested

including multiple drug-resistant clinical isolates, with MIC values ≤ 0.25 mg/L. Nosiheptide is also highly active

against Enterococcus spp and the contemporary hypervirulent BI strain of Clostridium difficile but is inactive against

most Gram-negative strains tested. Time-kill analysis reveals Nosiheptide to be rapidly bactericidal against

Staphylococcus aureus in a concentration- and time-dependent manner, with a nearly 2-log kill noted at 6 hours at

10X MIC. Furthermore, Nosiheptide is found to be non-cytotoxic against mammalian cells at >> 100X MIC, and its

anti-Staphylococcus aureus activity is not inhibited by 20% human serum. Notably, Nosiheptide exhibits a

significantly prolonged post-antibiotic effect against both healthcare- and community-associated Staphylococcus

aureus compared to vancomycin[1].

Nosiheptide (20 mg/kg; intraperitoneal injection; injected at 1 and 8 h post-infection; female CD1 mice) provids

significant protection against mortality. Ten out of 10 of the Nosiheptide-treated mice remains alive on day 3, while

6/10 of the controls died on day 1[1]. Animal Model: Eight week old female CD1 mice injected with HA-

Staphylococcus aureus strain Sanger 252[1]

[1]. Haste NM, et al. Activity of the thiopeptide antibiotic nosiheptide against contemporary strains of methicillin-

resistant Staphylococcus aureus. J Antibiot (Tokyo). 2012 Dec;65(12):593-8. [2]. Yu Y, et al. Nosiheptide biosynthesis

featuring a unique indole side ring formation on the characteristic thiopeptide framework. ACS Chem Biol. 2009 Oct

16;4(10):855-64.

Caution: Producthasnot been fully validated for medical applications. For research use only.

Tel: (626) 353-8530 Fax: (626) 353-8530 E-mail: tech@

Address: 10292 Central Ave. #205, Montclair, CA, USA

2024年11月3日发(作者:威聪)

Peptides, Inhibitors, Agonists

Product Data Sheet

Product Name:

Cat. No.:

Nosiheptide

GC38117

Chemical Properties

Cas No.

Chemical

Name

Canonical

SMILES

Formula

Solubility

General tips

Shipping

Condition

56377-79-8

N/A

OC1=C(C2=NC(C(NC(C(N)=O)=C)=O)=CS2)N=C(C3=CSC(C4NC(C5=CSC(C(CC(C(OCC6=C7C(C)=C(

NC7=CC=C6)C(SC4)=O)=O)O)NC(C8=CSC(/C(NC(C(C(O)C)NC(C9=CSC%10=N9)=O)=O)=CC)=N8)=

O)=N5)=O)=N3)C%10=C1

C

51

H

43

N

13

O

12

S

6

Soluble in DMSO

Storage

1222.36

Store at -20°C

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath

for a solution can be stored below -20℃ for several months.

Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon

request.

Structure

Background

Nosiheptide (Multhiomycin), a thiopeptide antibiotic produced by Streptomyces actuosus, inhibits bacterial protein

Caution: Producthasnot been fully validated for medical applications. For research use only.

Tel: (626) 353-8530 Fax: (626) 353-8530 E-mail: tech@

Address: 10292 Central Ave. #205, Montclair, CA, USA

Peptides, Inhibitors, Agonists

Product Data Sheet

synthesis and bears a unique indole side ring system and regiospecific hydroxyl groups on the characteristic

macrocyclic core. Nosiheptide has been widely used as a feed additive for animal growth[1][2].

Nosiheptide exhibits extremely potent activity against all contemporary Staphylococcus aureus strains tested

including multiple drug-resistant clinical isolates, with MIC values ≤ 0.25 mg/L. Nosiheptide is also highly active

against Enterococcus spp and the contemporary hypervirulent BI strain of Clostridium difficile but is inactive against

most Gram-negative strains tested. Time-kill analysis reveals Nosiheptide to be rapidly bactericidal against

Staphylococcus aureus in a concentration- and time-dependent manner, with a nearly 2-log kill noted at 6 hours at

10X MIC. Furthermore, Nosiheptide is found to be non-cytotoxic against mammalian cells at >> 100X MIC, and its

anti-Staphylococcus aureus activity is not inhibited by 20% human serum. Notably, Nosiheptide exhibits a

significantly prolonged post-antibiotic effect against both healthcare- and community-associated Staphylococcus

aureus compared to vancomycin[1].

Nosiheptide (20 mg/kg; intraperitoneal injection; injected at 1 and 8 h post-infection; female CD1 mice) provids

significant protection against mortality. Ten out of 10 of the Nosiheptide-treated mice remains alive on day 3, while

6/10 of the controls died on day 1[1]. Animal Model: Eight week old female CD1 mice injected with HA-

Staphylococcus aureus strain Sanger 252[1]

[1]. Haste NM, et al. Activity of the thiopeptide antibiotic nosiheptide against contemporary strains of methicillin-

resistant Staphylococcus aureus. J Antibiot (Tokyo). 2012 Dec;65(12):593-8. [2]. Yu Y, et al. Nosiheptide biosynthesis

featuring a unique indole side ring formation on the characteristic thiopeptide framework. ACS Chem Biol. 2009 Oct

16;4(10):855-64.

Caution: Producthasnot been fully validated for medical applications. For research use only.

Tel: (626) 353-8530 Fax: (626) 353-8530 E-mail: tech@

Address: 10292 Central Ave. #205, Montclair, CA, USA

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