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Art. -Nr.: HY-P10208

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RKH

Name: RKH
Brand: MedChemExpress
SKU: HY-P10208
Availability: PreOrder

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

RKH is an orally active tripeptide derived from Akkermansia muciniphila and a TLR4 inhibitor that binds to TLR4 with a K_d of 3.34 nM. RKH blocks LPS-induced TLR4/MD2 dimerization, inhibits LPS-induced proinflammatory cytokine expression and systemic inflammation, and exhibits stronger inhibition of TLR4-mediated cytokine expression than other TLR pathways in macrophages. RKH inhibits sepsis-induced systemic proinflammatory cytokine production as well as macrophage recruitment and proinflammatory activation. RKH prevents lethal sepsis and attenuates organ injury in mouse and piglet sepsis models. RKH can be used for research on sepsis.

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Formel: C₁₈H₃₃N₉O₄
Molecular Weight:439.51

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

RKH Chemical Structure

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Other In-stock Forms of RKH

RKH acetate

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

TLR4

3.34 nM (Kd)

Alle Endogenous Metabolite Isoform-spezifische Produkte anzeigen :

Alle Toll-like Receptor (TLR) Isoform-spezifische Produkte anzeigen :

In Vitro

Innate ImmunityCytokines & Chemokines

Innate Immunity

RKH directly binds TLR4 with a K_D of 3.34 nM in SPR^[1].
RKH (125 μM) protects TLR4 protein from pronase hydrolysis in vitro; and exerts a thermal stabilizing effect on TLR4 in macrophages across the 37-67 °C CETSA gradient range^[1].
RKH (125 μM; 15 min) inhibits LPS-induced TLR4 downstream P38, P65, JNK, and ERK signaling transduction in THP-1-dMs cells, thereby reducing LPS-induced pro-inflammatory factor expression in macrophages, with weak inhibitory effects on other TLRs^[1].
RKH (125 μM; 15 min) reduces the binding of FITC-LPS to BMDMs and THP-1-dMs without altering TLR4/MD2 expression or internalization^[1].
RKH inhibits LPS-induced TLR4-TLR4 and TLR4-MD2 dimerization in BMDMs and THP-1-dMs^[1].
RKH-mediated inhibition of TLR4 dimerization in THP-1-dMs requires ARG264, LEU293, ASP294, and LYS362 on TLR4^[1].

Innate Immunity

Cytokines & Chemokines

RKH inhibits LPS-induced Il-6, Il-1β, Ccl3, and Ccl4 mRNA in BMDMs and THP-1-dMs^[1].
RKH is a tripeptide produced by Akkermansia muciniphila that inhibits LPS-induced pro-inflammatory cytokine expression in BMDMs and THP-1-derived macrophages, and directly binds TLR4^[2].

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

Western Blot Analysis^[1]

Cell Line:

THP-1-dMs cells
Concentration:

125 μM
Incubation Time:

15 min
Result:

Inhibited LPS-induced TLR4 downstream P38, P65, JNK, and ERK signaling transduction in THP-1-dMs cells, thereby reducing LPS-induced pro-inflammatory factor expression in macrophages, with weak inhibitory effects on other TLRs.

In Vivo

Innate Immunity

RKH (50 mg/kg; intragastric administration; 2 h before LPS injection) pretreatment protects mice against CLP-induced lethal sepsis, organ injury, and systemic inflammation; and exerts no protective effect against CLP-induced lethal sepsis in TLR4 knockout mice^[1].
RKH (50 mg/kg; intragastric administration; 2 h before LPS injection) pretreatment protects mice from LPS-induced lethal sepsis and organ injury^[1].
RKH (1 mg/kg; intragastric administration; 2 h before LPS injection) pretreatment prolongs the survival time of LPS-induced septic piglets and alleviates excessive inflammation and organ injury^[1].
RKH pretreatment exerts a protective effect in septic mice by prolonging survival time and alleviating acute tissue injury and inflammation, and it also exerts a protective effect against sepsis in a septic piglet model^[2].

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

Animal Model:

C57BL/6 mice (mlae, 6-8 weeks, induced by CLP operation), TLR4 knockout (TLR4^-/-) mice^[1]
Dosage:

50 mg/kg
Administration:

intragastric administration; 2 h before LPS injection
Result:

Protected mice against CLP-induced lethal sepsis, organ injury, and systemic inflammation; and exerted no protective effect against CLP-induced lethal sepsis in TLR4 knockout mice.

Animal Model:

C57BL/6 mice (mlae, 6-8 weeks, induced by LPS administration)^[1]
Dosage:

50 mg/kg
Administration:

intragastric administration; 2 h before LPS injection
Result:

Protected mice from LPS-induced lethal sepsis and organ injury.

Animal Model:

piglet (induced by LPS administration, LPS (300 μg/kg) was injected intravenously for 30 min)^[1]
Dosage:

1 mg/kg
Administration:

intragastric administration; 2 h before LPS injection
Result:

Prolonged the survival time of LPS-induced septic piglets and alleviates excessive inflammation and organ injury.

Related Protocols :

Chemical Information

Molecular Weight 439.51
Formel C₁₈H₃₃N₉O₄
Sequence

Arg-Lys-His
Sequence Shortening

RKH
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (1)

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Journal Impact Factor

JCI Insight

CD4+ T helper 2 cell-macrophage crosstalk induces IL-24-mediated breast cancer suppression. [Abstract]

2025 Jan 9;10(1):e180962. PMID: 39782693

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Cani P D, et al. Akkermansia muciniphila derived tripeptide jams the gear of sepsis, inflammation and mortality. Gut, 2023.

[2]. Li L, et al. Function and therapeutic prospects of next-generation probiotic Akkermansia muciniphila in infectious diseases. Frontiers in Microbiology, 2024.

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Reinheit & Dokumentation
Verweise

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