Fig. 1 · Structure

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Anamorelin

Cat. No. A12346 CAS 249921-19-5

GHSR agonist

Anamorelin (ONO-7643, RC-1291, ST-1291) is an orally active, high-affinity, selective agonist of the ghrelin receptor with an EC50 value of 0.74 nM in the HEK293/GRLN FLIPR assay. Anamorelin is currently under development for the management of non-small lung cancer associated cachexia/anorexia.

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Publications for Anamorelin

1 publication citing this product

  1. Josua Jordi, .et al. , Sci Adv, 2018, Oct; 4(10): eaav1966 PMID: 30402545

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In Vivo Studies

In aged C57BL/6 mice, daily oral Anamorelin produced modest increases in body weight and fat mass compared with PBS-treated controls. In male non-cancer-bearing mice receiving Anamorelin by oral gavage, the reported body-weight comparison with vehicle controls was not statistically significant. In female athymic nude mice bearing A549 tumors, daily oral Anamorelin increased percentage body-weight change significantly at the higher tested doses compared with water controls, while the lowest tested dose did not. In tumor-bearing BALB/c mice, daily Anamorelin by oral gavage had no effect on tumor growth during treatment. [1,2,3]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Anamorelin and body weight in aged mice

Animal study · 23‐month‐old C57BL/6 mice [1]

Aged C57BL/6 mice received Anamorelin daily by oral administration. Treatment produced modest increases in body weight and fat mass compared with PBS-treated controls.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
body weightReported result anamorelin treatment resulted in a modest increase in body weight and fat mass in aged mice compared with PBS‐treated controls[1]

Conditions shared by the study groups

Route
p.o.
Treatment course
anamorelin (30 mg·kg−1 for 4 weeks) were administered daily p.o.
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Anamorelin 30 mg·kg−1PBS‐treated controlsanamorelin treatment resulted in a modest increase in body weight and fat mass in aged mice compared with PBS‐treated controls[1]
Anamorelin 30 mg·kg−1
Model: 23‐month‐old C57BL/6 mice
Reported limits: Not stated in the sentences used: vehicle.
Methods and source locations

Compound reported in the paper: Anamorelin

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Materials and Methods > Chemical Administration (S16, S19); Results > KARIs Attenuate Age‐Related Decline in Skeletal Muscle Mass and Function in Mice (S93)

body weight: body weight; comparator: PBS‐treated controls — Materials and Methods > Chemical Administration (S19); Results > KARIs Attenuate Age‐Related Decline in Skeletal Muscle Mass and Function in Mice (S93)

Anamorelin 30 mg·kg−1 · Materials and Methods > Chemical Administration (S19); Results > KARIs Attenuate Age‐Related Decline in Skeletal Muscle Mass and Function in Mice (S93)

Anamorelin and Body Weight in Non-Cancer-Bearing Mice

Animal study · Non-cancer-bearing mice; male C3H mice; Six mice were included in each treatment group [2]

Non-cancer-bearing male mice received Anamorelin by oral gavage, with vehicle-only animals as controls. The body-weight result was reported as non-significant.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Body Weight (gram)Reported result Body Weight (gram): 24.2 ± 0.8; n.s.[2]

Conditions shared by the study groups

Route
oral gavage
Treatment course
2 weeks; Day 14
Vehicle
200 μL sterile water
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Anamorelin 20 mg/kg/daynon-treated control (vehicle only)Body Weight (gram): 24.2 ± 0.8; n.s.[2]
Anamorelin 20 mg/kg/day
Model: Non-cancer-bearing mice; male C3H mice; Six mice were included in each treatment group
Reported limits: Removed after verification: value.
Methods and source locations

Compound reported in the paper: Anamorelin

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

4. Materials and Methods > 4.2. Animal Experiments (S51, S55, S57, S58, S59); Table 1 (T1.h1, T1.r2, T1.r3)

Body Weight (gram): Body Weight (gram); comparator: non-treated control (vehicle only) — Table 1 (T1.h1, T1.r2, T1.r3)

Anamorelin 20 mg/kg/day · 4. Materials and Methods > 4.2. Animal Experiments (S57, S58, S59); Table 1 (T1.h1, T1.r2, T1.r3)

Anamorelin and body weight in tumor-bearing nude mice

Animal study · female athymic nude mice (nu/nu, Harlan); A549 tumor cells; 15 mice each [3]

Female athymic nude mice bearing A549 tumors received Anamorelin orally once daily. The higher tested doses produced statistically significant increases in percentage body-weight change compared with water controls; the lowest tested dose did not.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Percentage change in BW from days 3 to 30percentage change in mean BW 30 mg/kg/day: 14.4 % ± 1.08[3]

Conditions shared by the study groups

Route
p.o.
Treatment course
From day 3 to day 30 (28-day treatment period); once daily
Vehicle
de-ionized (DI) water
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Anamorelin 3, 10, or 30 mg/kgDI water p.o.Over the treatment period, animals administered anamorelin at 10 and 30 mg/kg/day showed a statistically significant increase in their percentage of mean BW (11.7 % ± 1.26 and 14.4 % ± 1.08, respectively) compared with controls (7.6 % ± 0.99; p < 0.01 versus 10 mg/kg and p < 0.001 versus 30 mg/kg). Mice administered 3 mg/kg anamorelin did not show a statistically significant increase in BW compared with control animals (9.1 % ± 0.97; p > 0.05).[3]
Anamorelin 3, 10, or 30 mg/kg
Model: female athymic nude mice (nu/nu, Harlan); A549 tumor cells; 15 mice each
Methods and source locations

Compound reported in the paper: Anamorelin

Evidence for Anamorelin as the hydrochloride form reported in the paper, not the free base/neutral form supplied as A12346; no salt equivalence, dose conversion or lot validation.

Materials and methods > Test agents (S2); Materials and methods > Mice (S4); Materials and methods > Tumor cell culture and implantation (S9, S10); Materials and methods > Treatment study design (S12, S16); Materials and methods > Endpoints (S24); Results > Effects of ghrelin and anamorelin on food consumption and body weight (S48, S49)

Percentage change in BW from days 3 to 30: Percentage change in BW from days 3 to 30; comparator: DI water p.o. — Materials and methods > Endpoints (S24); Results > Effects of ghrelin and anamorelin on food consumption and body weight (S48, S49)

Anamorelin 3, 10, or 30 mg/kg · Materials and methods > Treatment study design (S16); Results > Effects of ghrelin and anamorelin on food consumption and body weight (S48, S49)

Tumor Growth in Colon Tumor-Bearing Mice

Animal study · 8‐week‐old BALB/c mice [1]

BALB/c mice bearing CT26 tumors received Anamorelin by oral gavage. Anamorelin had no effect on tumor growth during treatment compared with PBS-treated controls.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
tumour volumeReported result The administration of all doses of KARI compounds or anamorelin had no effect on tumour growth during the treatment period[1]

Conditions shared by the study groups

Route
oral gavage
Treatment course
Nine days after tumour inoculation, when tumours became measurable, mice were treated orally with PBS, KARI compounds (10 or 30 mg·kg−1) or anamorelin (30 mg·kg−1) daily until Day 24.
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Anamorelin 30 mg·kg−1CT26‐bearing mice treated with PBSThe administration of all doses of KARI compounds or anamorelin had no effect on tumour growth during the treatment period[1]
Anamorelin 30 mg·kg−1
Model: 8‐week‐old BALB/c mice
Reported limits: Not stated in the sentences used: vehicle.
Methods and source locations

Compound reported in the paper: Anamorelin

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Materials and Methods > Cancer Cachexia Mouse Model (S36, S38, S39, S40); Results > KARIs Improve Anorexia, Skeletal Muscle Loss and Functional Impairment in Cancer Cachexia Mice (S113, S114, S115)

tumour volume: tumour volume; comparator: CT26‐bearing mice treated with PBS — Materials and Methods > Cancer Cachexia Mouse Model (S40); Results > KARIs Improve Anorexia, Skeletal Muscle Loss and Functional Impairment in Cancer Cachexia Mice (S115)

Anamorelin 30 mg·kg−1 · Materials and Methods > Cancer Cachexia Mouse Model (S39); Results > KARIs Improve Anorexia, Skeletal Muscle Loss and Functional Impairment in Cancer Cachexia Mice (S113, S115)

Specifications

Manufacturer Adooq Bioscience
Actions Agonist
CAS Number 249921-19-5
Applications GHSR agonist
Formula C31H42N6O3
Molecular Weight 546.7
Synonyms ONO-7643; RC-1291; ST-1291
SMILES
CC(C)(C(=O)N[C@H](CC1=CNC2=CC=CC=C21)C(=O)N3CCC[C@](C3)(CC4=CC=CC=C4)C(=O)N(C)N(C)C)N

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 92 mg/mL (168.28 mM)
Water Insoluble
Ethanol 73 mg/mL (133.53 mM)

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Yoon HJ, Han WH, Kim SB, et al. KARIs, Ghrelin Receptor Agonists With Excellent Brain Permeability, Increase Food Intake and Attenuate the Muscle Loss in Mice. J Cachexia Sarcopenia Muscle (2026). PMID: 41923173 DOI: 10.1002/jcsm.70277 Source material
  2. [2] Miyake M, Hori S, Itami Y, et al. Supplementary Oral Anamorelin Mitigates Anorexia and Skeletal Muscle Atrophy Induced by Gemcitabine Plus Cisplatin Systemic Chemotherapy in a Mouse Model. Cancers (Basel) (2020). PMID: 32709007 DOI: 10.3390/cancers12071942 Source material
  3. [3] Northrup R, Kuroda K, Duus EM, et al. Effect of ghrelin and anamorelin (ONO-7643), a selective ghrelin receptor agonist, on tumor growth in a lung cancer mouse xenograft model. Support Care Cancer (2013). PMID: 23579947 DOI: 10.1007/s00520-013-1800-0 Source material

Publications

1 publication citing this product

  1. Josua Jordi, .et al. , Sci Adv, 2018, Oct; 4(10): eaav1966 PMID: 30402545

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